Oxadiazole derivatives have played a vital part in the development of heterocyclic compounds. In this present work, a series of 5-(2-aminophenyl)-1,3,4-oxadiazole-2(3H)-thione derivatives (1-10) have been synthesized by Mannich reaction. The reaction progress of the synthesized compounds was checked by TLC. The structures of the newly synthesized compounds were confirmed by IR and 1H NMR spectral data. The in-vitro anti-inflammatory activity of 1, 3, 4-oxadiazole compounds (1-10) was assessed by HRBC Membrane Stabilization Method. Among the newly synthesized 1,3,4-oxadiazole derivatives, compounds OFP, OAP, OBNP, OPBNP, ORP, OUP, OPClBP, OFD, OAD and OBND possessed highly significant anti-inflammatory activity at a dose of 1000µg/ml when compared with standard, Diclofenac potassium.
Multiple Method Development and Validation for Simultaneous Estimation of Chl...ijtsrd
A simple, precise and accurate multiple analytical method has been developed for the simultaneous estimation of Chlorzoxazone and Nimesulide in bulk and tablet formulations by reversed-phase liquid chromatographic and UV-Visible spectrophotometric techniques. The chromatographic separation was achieved on C18 analytical column. A mixture of Methanol 0.1 Ortho-phosphoric acid 75 25 was used as mobile phase, at a flow rate of 1mL min and detection wavelength at 295 nm. The retention time of Chlorzoxazone and Nimesulide was found to be 4.69 and 5.45 min respectively. The linear dynamic ranges for HPLC were from 2-10 µg mL and for simultaneous equation method, derivative spectroscopy, Q-ratio Absorbance method, Dual wavelength it was 10-30 µg mL for both Chlorzoxazone and Nimesulide. The percentage recovery obtained for Chlorzoxazone and Nimesulide were 100.93 and 102.19 respectively for RP-HPLC, 9.7 and 100.1 for simultaneous equation method of CZ and NIM respectively, 99.97 and 99.78 for derivative spectroscopy of CZ and NIM respectively, 101.37 and 99.48 for Q-ratio Absorbance method of CZ and NIM respectively, 100.13 and 99.96 for dual wavelength method of CZ and NIM respectively. The validation of the proposed methods were carried out for linearity, accuracy, precision, limit of detection, limit of quantitation and robustness. The developed method can be used for routine quality control analysis of titled drugs in combination in tablet formulation. Swetha Yarramsetti | A. Elphine Prabahar | Rama Rao Nadendla "Multiple Method Development and Validation for Simultaneous Estimation of Chlorzoxazone and Nimesulide in Bulk and Pharmaceutical Dosage Form" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-3 | Issue-2 , February 2019, URL: https://www.ijtsrd.com/papers/ijtsrd21503.pdf
Paper URL: https://www.ijtsrd.com/pharmacy/analytical-chemistry/21503/multiple-method-development-and-validation-for--simultaneous-estimation-of-chlorzoxazone-and--nimesulide-in-bulk-and-pharmaceutical-dosage-form/swetha-yarramsetti
Anthranilic acid on heating with a primary amide
resulted in benzamidomethyl/ phthalimidomethyl-quinazolin 4
(3H) ones (II) which on treatment with phosphorus oxychloride
(POCl3) and phosphorus pentachloride (PCl5) afforded 4-chloro-
2-benzamidomethyl/phthalimidomethyl-quinazolines (III).
Reaction of (III) with o-phenylenediamine in anhydrous pyridine
furnished 2-benzamidomethyl/ phthalimido-methylbenzimidazolo
[2, 1-c] quinazolines (IV). A part of synthetic
strategy was also adopted for the synthesis of 2-
benzamidomethyl/ phthalimidomethyl-tetrazolo [1, 5-c]
quinazolines (V) with the interaction of (III) with sodium azide
(NaN3) indimethyl sulphoxide (DMSO) solvent (Scheme)
Spectrophotometric Determination of Cardiovascular DrugsIJMER
International Journal of Modern Engineering Research (IJMER) is Peer reviewed, online Journal. It serves as an international archival forum of scholarly research related to engineering and science education.
Determination of Satranidazole through Ion-Associative Complex ReactionRatnakaram Venkata Nadh
A simple, selective, accurate and low-cost spectrophotometric method
has been described for determination of satranidazole in bulk and
pharmaceutical formulations. The developed method involves the
formation of chloroform extractable colored ion-association complex
of satranidazole with Tropaeolin OOO (TPooo). The extracted colored
complex showed absorbance maximum at wavelength 484 nm and
obeying Beer′s law in the concentration 4-20 μg mL-1 with the
correlation coeffiecent of 0.9998. The results of statistical analysis of
the proposed method reveals high accuracy and good precession. Thus,
the proposed method can be used commercially for the determination
of satranidazole in bulk and pharmaceutical formulations.
New spectrophotometric methods for the quantitative estimation of oxolamine i...IJSIT Editor
Five simple, sensitive and economical spectrophotometric methods have been developed for the
determination of Oxolamine in commercial dosage forms. The methods were based on the formation of
colored complex of Oxolamine with different reagents. The absorbance of the formed color complex is
measured at the wavelength of maximum absorbance of the complex against the reagent blank treated
similarly. All these method have different linearity ranges. Statistical analysis proves that the proposed
methods are reproducible and selective for the estimation of Oxolamine in bulk drug and in its tablet dosage
form.
ER Publication,
IJETR, IJMCTR,
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International Journals,
High Impact Journals,
Monthly Journal,
Good quality Journals,
Research,
Research Papers,
Research Article,
Free Journals, Open access Journals,
erpublication.org,
Engineering Journal,
Science Journals,
Multiple Method Development and Validation for Simultaneous Estimation of Chl...ijtsrd
A simple, precise and accurate multiple analytical method has been developed for the simultaneous estimation of Chlorzoxazone and Nimesulide in bulk and tablet formulations by reversed-phase liquid chromatographic and UV-Visible spectrophotometric techniques. The chromatographic separation was achieved on C18 analytical column. A mixture of Methanol 0.1 Ortho-phosphoric acid 75 25 was used as mobile phase, at a flow rate of 1mL min and detection wavelength at 295 nm. The retention time of Chlorzoxazone and Nimesulide was found to be 4.69 and 5.45 min respectively. The linear dynamic ranges for HPLC were from 2-10 µg mL and for simultaneous equation method, derivative spectroscopy, Q-ratio Absorbance method, Dual wavelength it was 10-30 µg mL for both Chlorzoxazone and Nimesulide. The percentage recovery obtained for Chlorzoxazone and Nimesulide were 100.93 and 102.19 respectively for RP-HPLC, 9.7 and 100.1 for simultaneous equation method of CZ and NIM respectively, 99.97 and 99.78 for derivative spectroscopy of CZ and NIM respectively, 101.37 and 99.48 for Q-ratio Absorbance method of CZ and NIM respectively, 100.13 and 99.96 for dual wavelength method of CZ and NIM respectively. The validation of the proposed methods were carried out for linearity, accuracy, precision, limit of detection, limit of quantitation and robustness. The developed method can be used for routine quality control analysis of titled drugs in combination in tablet formulation. Swetha Yarramsetti | A. Elphine Prabahar | Rama Rao Nadendla "Multiple Method Development and Validation for Simultaneous Estimation of Chlorzoxazone and Nimesulide in Bulk and Pharmaceutical Dosage Form" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-3 | Issue-2 , February 2019, URL: https://www.ijtsrd.com/papers/ijtsrd21503.pdf
Paper URL: https://www.ijtsrd.com/pharmacy/analytical-chemistry/21503/multiple-method-development-and-validation-for--simultaneous-estimation-of-chlorzoxazone-and--nimesulide-in-bulk-and-pharmaceutical-dosage-form/swetha-yarramsetti
Anthranilic acid on heating with a primary amide
resulted in benzamidomethyl/ phthalimidomethyl-quinazolin 4
(3H) ones (II) which on treatment with phosphorus oxychloride
(POCl3) and phosphorus pentachloride (PCl5) afforded 4-chloro-
2-benzamidomethyl/phthalimidomethyl-quinazolines (III).
Reaction of (III) with o-phenylenediamine in anhydrous pyridine
furnished 2-benzamidomethyl/ phthalimido-methylbenzimidazolo
[2, 1-c] quinazolines (IV). A part of synthetic
strategy was also adopted for the synthesis of 2-
benzamidomethyl/ phthalimidomethyl-tetrazolo [1, 5-c]
quinazolines (V) with the interaction of (III) with sodium azide
(NaN3) indimethyl sulphoxide (DMSO) solvent (Scheme)
Spectrophotometric Determination of Cardiovascular DrugsIJMER
International Journal of Modern Engineering Research (IJMER) is Peer reviewed, online Journal. It serves as an international archival forum of scholarly research related to engineering and science education.
Determination of Satranidazole through Ion-Associative Complex ReactionRatnakaram Venkata Nadh
A simple, selective, accurate and low-cost spectrophotometric method
has been described for determination of satranidazole in bulk and
pharmaceutical formulations. The developed method involves the
formation of chloroform extractable colored ion-association complex
of satranidazole with Tropaeolin OOO (TPooo). The extracted colored
complex showed absorbance maximum at wavelength 484 nm and
obeying Beer′s law in the concentration 4-20 μg mL-1 with the
correlation coeffiecent of 0.9998. The results of statistical analysis of
the proposed method reveals high accuracy and good precession. Thus,
the proposed method can be used commercially for the determination
of satranidazole in bulk and pharmaceutical formulations.
New spectrophotometric methods for the quantitative estimation of oxolamine i...IJSIT Editor
Five simple, sensitive and economical spectrophotometric methods have been developed for the
determination of Oxolamine in commercial dosage forms. The methods were based on the formation of
colored complex of Oxolamine with different reagents. The absorbance of the formed color complex is
measured at the wavelength of maximum absorbance of the complex against the reagent blank treated
similarly. All these method have different linearity ranges. Statistical analysis proves that the proposed
methods are reproducible and selective for the estimation of Oxolamine in bulk drug and in its tablet dosage
form.
ER Publication,
IJETR, IJMCTR,
Journals,
International Journals,
High Impact Journals,
Monthly Journal,
Good quality Journals,
Research,
Research Papers,
Research Article,
Free Journals, Open access Journals,
erpublication.org,
Engineering Journal,
Science Journals,
Spectrophotometric Determination of Drugs and Pharmaceuticals by Cerium (IV) ...IOSR Journals
Simple, sensitive, accurate, and precise spectrophotometric methods for quantitative determination of drugs, viz., Darifenacin (DAR), Esmolol Hydrochloride (ESM), Montelukast Sodium (MON), Sildenafil citrate (SIL),Terbinafine (TER) and Tramadol Hydrochloride (TRA) were developed. The method of each drug depends upon oxidation of drugs by Ce (IV) (Excess) and estimating the amount of unreacted Ce (IV) by amaranth dye at 523nm. The calibration curves obeyed Beer’s law over the concentration range of 1.4-7.0 μg ml-1 (DAR), 2-14 μg ml-1 (ESM), 2-10 μg ml-1 (MON), 20-70 μg ml-1 (SIL), 3-21 μg ml-1 (TER) & 2-14 μg ml-1 (TRA). The methods have been validated in terms of guidelines of ICH and applied to analysis of pharmaceuticals.
Kinetic Spectrophotometric Determination of Drugs Based On Oxidation by Alkal...IOSR Journals
Simple, accurate and precise spectrophotometic methods for quantitative determination of four drugs viz., Levofloxacin (LEV), Moxifloxacin (MOX), Pseudo Ephidrine (PSE), Torsemide (TOR) have been developed based on oxidation of the drugs by alk.KMnO4. Kinetics of the oxidation reaction is followed spectrophotometrically, as one of the reaction product, Mn(VI), absorbed at 610 nm. Initial rate and fixed time method are used for the construction of calibration curves Beer’s law is obeyed in the range 6.25-37.5 μg ml-1 for LEV; 5-30 μg ml-1 for MOX; 6.25-37.5 μg ml-1 for PSE and 2.5-15 μg ml-1 for TOR. Recovery studies using pure samples and pharmulations in the Beer’s Law limits have been carried out. Excellent recoveries indicate the methods are accurate and precise. The methods have been validated in terms of ICH guidelines. Statistical analysis in terms of student’s t- test and variance F- tests demonstrate high accuracy and precision and suggest the methods can be applied in bulk drug and pharmaceutical industries.
Department of Pharmaceutical Management and Regulatory Affairs, Lachoo Memorial College of Science & Technology, Pharmacy Wing, Jodhpur National University, Rajasthan – 342003
Synthesis, Anticonvulsant Activity and Cytotoxicity of Novel Valproic Acid De...IOSRJAC
Objective: The aim of this work was to construct novel hydrazones and thiosemsicarbazide derivatives of valproic acid. The new targets will be evaluated for their anticonvulsant activity and cytotoxicity effects. Methods:Targets 7a-k, 10. 11 were synthesized starting from valproic acid using benzotriazole activation and hydrazide and thiosemicarbazide chemistry. The anticonvulsant activity was evaluated by pentylenetetrazoleinduced seizures modes using sodium valproate as a standard for comparison of the activity. The compounds with high anticonvulsant activity were subsequently examined for cytotoxicity against HepG2 by MTT assay. Results:The new targets were characterized using 1HNMR and 13CNMR and their purity were authenticated by elemental analysis. Four compounds 7e, 7j, 10 and 11exhibited the most potent anticonvulsant activity associated with low cytotixicity. Conclusion: Compounds 11 exhibited a moderate anticonvulsant activity and a significantly lower cytotoxicity than valproic acid and 5-fluorouracile suggesting that it could be used as a lead for the development of better anticonvulsant drug candidates.
A new analytical method development and validation for the simultaneus estima...SriramNagarajan19
A simple and selective LC method is described for the determination of Albuterol and Ipratropium Bromide in tablet dosage forms. Chromatographic separation was achieved on a c18 column using mobile phase consisting of a mixture of 80 volumes of methanol and 20 volumes of water with detection of 239 nm. Linearity was observed in the range 36-84 µg /ml for Albuterol (r2 =0.996) and 6-14 µg /ml for Ipratropium Bromide (r2 =0.997) for the amount of drugs estimated by the proposed methods was in good agreement with the label claim.
The proposed methods were validated. The accuracy of the methods was assessed by recovery studies at three different levels. Recovery experiments indicated the absence of interference from commonly encountered pharmaceutical additives. The method was found to be precise as indicated by the repeatability analysis, showing %RSD less than 2. All statistical data proves validity of the methods and can be used for routine analysis of pharmaceutical dosage form.
Design, synthesis, characterization and biological evaluation of 3- (4-(7-chl...iosrjce
Novel thiazolidinone derivatives TQ-VI(1-10) were designed, synthesized and screened for
antimicrobial activity. Synthesis of 3-(4-(7-chloro-2-(4-chlorophenyl) 4-oxo-quinazolin-3(4H)-yl) phenyl) -
2-arylthiazolidin-4-one TQ-VI(1-10) have been achieved from the starting material 2-amino-4-chlorobenzoic
acid TQ-I on cyclization with p-chlorobenzoyl chloride TQ-II to yield 7-chloro-2-(4-chlorophenyl)-4H-3,1-
benzoxazin-4-one,TQ-III, which on treatment with p-phenylindiamine gave 3-(4-aminophenyl)-7-chloro-2-(4-
chlorophenyl)quinazolin-4(3H)-one, TQ-IV in good yield. Then, TQ-IV on reaction with substituted aromatic
aldehydes converted to TQ-V(1-10), which on cyclization with thioglycolic acid gave TQ-VI (1-10). All the
synthesized compounds have been characterized on the basis of IR,
1
H-NMR and mass spectral data. The
compounds containing 4-OH, 4-OCH3 and 3,4,5-(OCH3)3 showed good activity. The title compounds were
screened for qualitative (zone of inhibition) and quantitative antimicrobial activity (MIC) by agar cup plate
method and serial dilution technique, respectively. Among the synthesized compounds in the series, the
compound TQVI4 and TQVI5 were found to exhibit significant antifungal activity at lower concentration of
31.25 µg/ml, against A.niger. The compound TQVI5 and TQVI4 showed zone of inhibition of 17mm and 15mm
against A.niger and C.albicans respectively which is comparable to that of standard drug. The rest of the
analogues in the series displayed weak to moderate antimicrobial activity when compared to the standard
positive controls Ampicillin and Amphotericin B.
An Efficient Synthetic Approach Towards 4-Cyano-3-(Methylthio)-5-Oxo-2H-Pyraz...inventionjournals
ABSTRACT: Synthesis of novel heterocyclic 4-cyano -3-(methylthio)-5-oxo-2H-pyrazole-1(5H)- carbothioamide (3) was prepared by condensing ethyl-2-cyano-3,3-bis (methylthio)acrylate (1) with thiosemicarbazide (2) in DMF and catalytic amount of potassium carbonate. Compound (3) has methylthio group at third position, which is replaced by different nucleophiles such as substituted anilines| phenols| hetryl amines| compounds containing active methylene group to afford 3-substituted derivatives of compound (3). All the newly synthesized compounds were screened for their antimicrobial activity.
Various human diseases have oxidative stress as one of their component. Many herbs have been reported to exhibit properties that combat oxidative stress through their active constituents such as flavonoids, tannins, phenolic compounds etc. Different Plants of Dillenicea family has been shown in in vitro experiments to be endowed with antioxidant activity. Therefore this study was carried out to evaluate Dillenicea family for its antioxidant activity.
Analytical method development and validation for the estimation of quinapril ...SriramNagarajan19
A simple and selective LC method is described for the determination of Quinapril and Tolcapone tablet dosage forms. Chromatographic separation was achieved on a c18 column using mobile phase consisting of a Mixed Phosphate buffer (KH2PO4 +K2HPO4): Acetonitrile 40:60, with detection of 239 nm. Linearity was observed in the range 50 - 150 µg /ml for Quinapril (r2 =0.995) and 62.5- 187.5µg /ml for Tolcapone (r2 =0.999) for the amount of drugs estimated by the proposed methods was in good agreement with the label claim.
The proposed methods were validated. The accuracy of the methods was assessed by recovery studies at three different levels. Recovery experiments indicated the absence of interference from commonly encountered pharmaceutical additives. The method was found to be precise as indicated by the repeatability analysis, showing %RSD less than 2. All statistical data proves validity of the methods and can be used for routine analysis of pharmaceutical dosage form.
N-alkylation methods, Characterization and Evaluation of antibacterial activi...IJERA Editor
A series of new 5-Chloroisatin derivates have been synthesized by the method of N-alkylation at room temperature, in the presence of a base and a catalyst with good yields. The chemical structures of these compounds were confirmed by NMR (1H &13C), these new compounds obtained were evaluated for their antibacterial activity. The final results revealed that the majority of the compounds exhibited good antimicrobial activity against various organisms
STUDY OF MPS UNDER STRESSED CONDITIONSvivatechijri
This study is done to access the chemical stability of the candidate compound in the pharmaceuticals.
Usually, it is performed at the preliminary stage in the process of drug development. Forced degradation/ stress
testing is performed under accelerated environment. The experimental conditions cause the candidate compound
to degrade under extreme conditions like acid and base hydrolysis, peroxide oxidation, photo-oxidation and
thermal stability to identify the resultant degradation products. This helps to establish degradation pathways and
thus intrinsic stability of a drug substance. The stability of product describes shelf life and storage conditions and
helps in the selection of appropriate formulations and their suitable packaging. This is compulsory for regulatory
documentation. The commonly used analytical approach for FDS is HPLC with UV and/ or MS but these
techniques consume a lot of time and not provide high resolution to confirm the precise detection of degradation
products. Use of UPLC with photodiode array and MS analysis supports the identification of degradation
products and also reduces the time needed to evolve stability indicating methods.
International Journal of Pharmaceutical Science Invention (IJPSI) is an international journal intended for professionals and researchers in all fields of Pahrmaceutical Science. IJPSI publishes research articles and reviews within the whole field Pharmacy and Pharmaceutical Science, new teaching methods, assessment, validation and the impact of new technologies and it will continue to provide information on the latest trends and developments in this ever-expanding subject. The publications of papers are selected through double peer reviewed to ensure originality, relevance, and readability. The articles published in our journal can be accessed online.
Synthesis and antimicrobial activity of some methyl (4- (benzo[d]oxazol-2-yl)...QUESTJOURNAL
ABSTRACT: In the present study, a new series of methyl (4-(benzo[d]oxazol-2-yl)phenyl) carbamodithioate amine derived from methyl (4-(benzo[d]oxazol-2-yl)phenyl) carbamodithioate (4TO1-TO6) have been synthesized by reacting the thio methyl group with different amines in presence of ethenol. The structural assessment of the compounds (TO 1- TO 6) was made on the basis of spectral data. The synthesized compounds were screened for their in vitro growth inhibiting activity against different strains of bacteria and fungi viz., Escherichia coli, Bacillus subtilis, Pseudomonas aeruginosa, S. aureus, Candida albicans and Cryptococcus neoformans were compared with standard agents such as Norfloxacin (10μg/ml) and Amphotericin B (10μg/ml) using broth dilution method. Compounds exhibit moderate to high antibacterial and antifungal activity
Simple and Eco-friendly Synthesis of Glycosides bearing triazolo[3,4-b][1,3,4...IOSRJAC
There is a vast variety of naturally occurring glycosides which have marked pharmacological properties. These glycosides have widely diversed functional groups modifications which result in influencing pharmacological performance of corresponding glycosides. The 3,6-disubstituted-s-triazolo[3,4- b][1,3,4]thiadiazoles were glucosidated with 2,3,4,6tetra-o-acetyl α D glulopryanosyl bromide using simple methodologies. The compounds obtained in good yield in a 80-90 minutes.
Synthesis, Characterization and Study of Antioxidant Activities of Some New P...IJRES Journal
A series of substituted pyrazoline derivatives 5(a-c) have been synthesized by the reaction of substituted chalcones 4(a-c) with isatinhydrazide. The starting materials, chalcones were prepared by clasien schimidt condensation of appropriate 1-hydroxy-2-acetonaphthone with substituted aldehydes in the presence of sodium hydroxide and in poly ethylene glycol (PEG-400). The structures of the synthesized compounds were confirmed by IR, 1HNMR & Mass spectral data. The synthesized compounds were screened for Antioxidant Activity by DPPH method.
ABSTRACT- L-Ascorbic acid derivatives was synthesized on treatment with acetone and acetyl chloride afforded 5,6-acetal of L-ascorbic acid then benzylation of C-2 and C-3 hydroxyl groups of the lactone ring was accomplished using K2CO3 and benzyl bromide in DMF, then deblocking of the 5,6-O,O-protected derivative of L-Ascorbic acid with acetic acid and methanol gave 2,3-O,O-dibenzyl-L-Ascorbic acid. Subsequently mono-tosylation at 6 position of 2,3-O, O-dibenzyl-L-Ascorbic acid was carried out with addition of p-toluenetosylchloride (PTSC) in Pyridine and MDC solvent medium gave 2,3-O,O-dibenzyl-6-O-tosyl-L-Ascorbic acid. All the structures were characterized by 1H NMR, 13C NMR and Mass Spectroscopy.
Key-words- L-Ascorbic acid, 5,6-Acetal, Benzylation, Hydrolysis, Tosylation
Spectrophotometric Determination of Drugs and Pharmaceuticals by Cerium (IV) ...IOSR Journals
Simple, sensitive, accurate, and precise spectrophotometric methods for quantitative determination of drugs, viz., Darifenacin (DAR), Esmolol Hydrochloride (ESM), Montelukast Sodium (MON), Sildenafil citrate (SIL),Terbinafine (TER) and Tramadol Hydrochloride (TRA) were developed. The method of each drug depends upon oxidation of drugs by Ce (IV) (Excess) and estimating the amount of unreacted Ce (IV) by amaranth dye at 523nm. The calibration curves obeyed Beer’s law over the concentration range of 1.4-7.0 μg ml-1 (DAR), 2-14 μg ml-1 (ESM), 2-10 μg ml-1 (MON), 20-70 μg ml-1 (SIL), 3-21 μg ml-1 (TER) & 2-14 μg ml-1 (TRA). The methods have been validated in terms of guidelines of ICH and applied to analysis of pharmaceuticals.
Kinetic Spectrophotometric Determination of Drugs Based On Oxidation by Alkal...IOSR Journals
Simple, accurate and precise spectrophotometic methods for quantitative determination of four drugs viz., Levofloxacin (LEV), Moxifloxacin (MOX), Pseudo Ephidrine (PSE), Torsemide (TOR) have been developed based on oxidation of the drugs by alk.KMnO4. Kinetics of the oxidation reaction is followed spectrophotometrically, as one of the reaction product, Mn(VI), absorbed at 610 nm. Initial rate and fixed time method are used for the construction of calibration curves Beer’s law is obeyed in the range 6.25-37.5 μg ml-1 for LEV; 5-30 μg ml-1 for MOX; 6.25-37.5 μg ml-1 for PSE and 2.5-15 μg ml-1 for TOR. Recovery studies using pure samples and pharmulations in the Beer’s Law limits have been carried out. Excellent recoveries indicate the methods are accurate and precise. The methods have been validated in terms of ICH guidelines. Statistical analysis in terms of student’s t- test and variance F- tests demonstrate high accuracy and precision and suggest the methods can be applied in bulk drug and pharmaceutical industries.
Department of Pharmaceutical Management and Regulatory Affairs, Lachoo Memorial College of Science & Technology, Pharmacy Wing, Jodhpur National University, Rajasthan – 342003
Synthesis, Anticonvulsant Activity and Cytotoxicity of Novel Valproic Acid De...IOSRJAC
Objective: The aim of this work was to construct novel hydrazones and thiosemsicarbazide derivatives of valproic acid. The new targets will be evaluated for their anticonvulsant activity and cytotoxicity effects. Methods:Targets 7a-k, 10. 11 were synthesized starting from valproic acid using benzotriazole activation and hydrazide and thiosemicarbazide chemistry. The anticonvulsant activity was evaluated by pentylenetetrazoleinduced seizures modes using sodium valproate as a standard for comparison of the activity. The compounds with high anticonvulsant activity were subsequently examined for cytotoxicity against HepG2 by MTT assay. Results:The new targets were characterized using 1HNMR and 13CNMR and their purity were authenticated by elemental analysis. Four compounds 7e, 7j, 10 and 11exhibited the most potent anticonvulsant activity associated with low cytotixicity. Conclusion: Compounds 11 exhibited a moderate anticonvulsant activity and a significantly lower cytotoxicity than valproic acid and 5-fluorouracile suggesting that it could be used as a lead for the development of better anticonvulsant drug candidates.
A new analytical method development and validation for the simultaneus estima...SriramNagarajan19
A simple and selective LC method is described for the determination of Albuterol and Ipratropium Bromide in tablet dosage forms. Chromatographic separation was achieved on a c18 column using mobile phase consisting of a mixture of 80 volumes of methanol and 20 volumes of water with detection of 239 nm. Linearity was observed in the range 36-84 µg /ml for Albuterol (r2 =0.996) and 6-14 µg /ml for Ipratropium Bromide (r2 =0.997) for the amount of drugs estimated by the proposed methods was in good agreement with the label claim.
The proposed methods were validated. The accuracy of the methods was assessed by recovery studies at three different levels. Recovery experiments indicated the absence of interference from commonly encountered pharmaceutical additives. The method was found to be precise as indicated by the repeatability analysis, showing %RSD less than 2. All statistical data proves validity of the methods and can be used for routine analysis of pharmaceutical dosage form.
Design, synthesis, characterization and biological evaluation of 3- (4-(7-chl...iosrjce
Novel thiazolidinone derivatives TQ-VI(1-10) were designed, synthesized and screened for
antimicrobial activity. Synthesis of 3-(4-(7-chloro-2-(4-chlorophenyl) 4-oxo-quinazolin-3(4H)-yl) phenyl) -
2-arylthiazolidin-4-one TQ-VI(1-10) have been achieved from the starting material 2-amino-4-chlorobenzoic
acid TQ-I on cyclization with p-chlorobenzoyl chloride TQ-II to yield 7-chloro-2-(4-chlorophenyl)-4H-3,1-
benzoxazin-4-one,TQ-III, which on treatment with p-phenylindiamine gave 3-(4-aminophenyl)-7-chloro-2-(4-
chlorophenyl)quinazolin-4(3H)-one, TQ-IV in good yield. Then, TQ-IV on reaction with substituted aromatic
aldehydes converted to TQ-V(1-10), which on cyclization with thioglycolic acid gave TQ-VI (1-10). All the
synthesized compounds have been characterized on the basis of IR,
1
H-NMR and mass spectral data. The
compounds containing 4-OH, 4-OCH3 and 3,4,5-(OCH3)3 showed good activity. The title compounds were
screened for qualitative (zone of inhibition) and quantitative antimicrobial activity (MIC) by agar cup plate
method and serial dilution technique, respectively. Among the synthesized compounds in the series, the
compound TQVI4 and TQVI5 were found to exhibit significant antifungal activity at lower concentration of
31.25 µg/ml, against A.niger. The compound TQVI5 and TQVI4 showed zone of inhibition of 17mm and 15mm
against A.niger and C.albicans respectively which is comparable to that of standard drug. The rest of the
analogues in the series displayed weak to moderate antimicrobial activity when compared to the standard
positive controls Ampicillin and Amphotericin B.
An Efficient Synthetic Approach Towards 4-Cyano-3-(Methylthio)-5-Oxo-2H-Pyraz...inventionjournals
ABSTRACT: Synthesis of novel heterocyclic 4-cyano -3-(methylthio)-5-oxo-2H-pyrazole-1(5H)- carbothioamide (3) was prepared by condensing ethyl-2-cyano-3,3-bis (methylthio)acrylate (1) with thiosemicarbazide (2) in DMF and catalytic amount of potassium carbonate. Compound (3) has methylthio group at third position, which is replaced by different nucleophiles such as substituted anilines| phenols| hetryl amines| compounds containing active methylene group to afford 3-substituted derivatives of compound (3). All the newly synthesized compounds were screened for their antimicrobial activity.
Various human diseases have oxidative stress as one of their component. Many herbs have been reported to exhibit properties that combat oxidative stress through their active constituents such as flavonoids, tannins, phenolic compounds etc. Different Plants of Dillenicea family has been shown in in vitro experiments to be endowed with antioxidant activity. Therefore this study was carried out to evaluate Dillenicea family for its antioxidant activity.
Analytical method development and validation for the estimation of quinapril ...SriramNagarajan19
A simple and selective LC method is described for the determination of Quinapril and Tolcapone tablet dosage forms. Chromatographic separation was achieved on a c18 column using mobile phase consisting of a Mixed Phosphate buffer (KH2PO4 +K2HPO4): Acetonitrile 40:60, with detection of 239 nm. Linearity was observed in the range 50 - 150 µg /ml for Quinapril (r2 =0.995) and 62.5- 187.5µg /ml for Tolcapone (r2 =0.999) for the amount of drugs estimated by the proposed methods was in good agreement with the label claim.
The proposed methods were validated. The accuracy of the methods was assessed by recovery studies at three different levels. Recovery experiments indicated the absence of interference from commonly encountered pharmaceutical additives. The method was found to be precise as indicated by the repeatability analysis, showing %RSD less than 2. All statistical data proves validity of the methods and can be used for routine analysis of pharmaceutical dosage form.
N-alkylation methods, Characterization and Evaluation of antibacterial activi...IJERA Editor
A series of new 5-Chloroisatin derivates have been synthesized by the method of N-alkylation at room temperature, in the presence of a base and a catalyst with good yields. The chemical structures of these compounds were confirmed by NMR (1H &13C), these new compounds obtained were evaluated for their antibacterial activity. The final results revealed that the majority of the compounds exhibited good antimicrobial activity against various organisms
STUDY OF MPS UNDER STRESSED CONDITIONSvivatechijri
This study is done to access the chemical stability of the candidate compound in the pharmaceuticals.
Usually, it is performed at the preliminary stage in the process of drug development. Forced degradation/ stress
testing is performed under accelerated environment. The experimental conditions cause the candidate compound
to degrade under extreme conditions like acid and base hydrolysis, peroxide oxidation, photo-oxidation and
thermal stability to identify the resultant degradation products. This helps to establish degradation pathways and
thus intrinsic stability of a drug substance. The stability of product describes shelf life and storage conditions and
helps in the selection of appropriate formulations and their suitable packaging. This is compulsory for regulatory
documentation. The commonly used analytical approach for FDS is HPLC with UV and/ or MS but these
techniques consume a lot of time and not provide high resolution to confirm the precise detection of degradation
products. Use of UPLC with photodiode array and MS analysis supports the identification of degradation
products and also reduces the time needed to evolve stability indicating methods.
International Journal of Pharmaceutical Science Invention (IJPSI) is an international journal intended for professionals and researchers in all fields of Pahrmaceutical Science. IJPSI publishes research articles and reviews within the whole field Pharmacy and Pharmaceutical Science, new teaching methods, assessment, validation and the impact of new technologies and it will continue to provide information on the latest trends and developments in this ever-expanding subject. The publications of papers are selected through double peer reviewed to ensure originality, relevance, and readability. The articles published in our journal can be accessed online.
Synthesis and antimicrobial activity of some methyl (4- (benzo[d]oxazol-2-yl)...QUESTJOURNAL
ABSTRACT: In the present study, a new series of methyl (4-(benzo[d]oxazol-2-yl)phenyl) carbamodithioate amine derived from methyl (4-(benzo[d]oxazol-2-yl)phenyl) carbamodithioate (4TO1-TO6) have been synthesized by reacting the thio methyl group with different amines in presence of ethenol. The structural assessment of the compounds (TO 1- TO 6) was made on the basis of spectral data. The synthesized compounds were screened for their in vitro growth inhibiting activity against different strains of bacteria and fungi viz., Escherichia coli, Bacillus subtilis, Pseudomonas aeruginosa, S. aureus, Candida albicans and Cryptococcus neoformans were compared with standard agents such as Norfloxacin (10μg/ml) and Amphotericin B (10μg/ml) using broth dilution method. Compounds exhibit moderate to high antibacterial and antifungal activity
Simple and Eco-friendly Synthesis of Glycosides bearing triazolo[3,4-b][1,3,4...IOSRJAC
There is a vast variety of naturally occurring glycosides which have marked pharmacological properties. These glycosides have widely diversed functional groups modifications which result in influencing pharmacological performance of corresponding glycosides. The 3,6-disubstituted-s-triazolo[3,4- b][1,3,4]thiadiazoles were glucosidated with 2,3,4,6tetra-o-acetyl α D glulopryanosyl bromide using simple methodologies. The compounds obtained in good yield in a 80-90 minutes.
Synthesis, Characterization and Study of Antioxidant Activities of Some New P...IJRES Journal
A series of substituted pyrazoline derivatives 5(a-c) have been synthesized by the reaction of substituted chalcones 4(a-c) with isatinhydrazide. The starting materials, chalcones were prepared by clasien schimidt condensation of appropriate 1-hydroxy-2-acetonaphthone with substituted aldehydes in the presence of sodium hydroxide and in poly ethylene glycol (PEG-400). The structures of the synthesized compounds were confirmed by IR, 1HNMR & Mass spectral data. The synthesized compounds were screened for Antioxidant Activity by DPPH method.
ABSTRACT- L-Ascorbic acid derivatives was synthesized on treatment with acetone and acetyl chloride afforded 5,6-acetal of L-ascorbic acid then benzylation of C-2 and C-3 hydroxyl groups of the lactone ring was accomplished using K2CO3 and benzyl bromide in DMF, then deblocking of the 5,6-O,O-protected derivative of L-Ascorbic acid with acetic acid and methanol gave 2,3-O,O-dibenzyl-L-Ascorbic acid. Subsequently mono-tosylation at 6 position of 2,3-O, O-dibenzyl-L-Ascorbic acid was carried out with addition of p-toluenetosylchloride (PTSC) in Pyridine and MDC solvent medium gave 2,3-O,O-dibenzyl-6-O-tosyl-L-Ascorbic acid. All the structures were characterized by 1H NMR, 13C NMR and Mass Spectroscopy.
Key-words- L-Ascorbic acid, 5,6-Acetal, Benzylation, Hydrolysis, Tosylation
Synthesis, Characterization, and Antibacterial Activity of Some Novel 5-Chlor...IJERA Editor
The development of potential antibacterial requires the synthesis of a new series of 5- Chloroisatin derivatives incorporating various aromatic aldehydes in the case 1,3-Dipolar Cycloaddition including Nitrile oxide, as well as the cycloaddition Alcyne-Azide Catalytic with Copper. The charcterization of the structure of the synthesized compounds was confirmed by means of their IR, 1H-NMR and 13C-NMR spectral data. In addition, the antibacterial properties in vitro were tested against certain microorganisms using the disk diffusion technique. A majority of compounds show better activity against several of the microorganisms.
Facial and Simple Synthesis of Some New (Pyrazole and Triazole) Coumarin Deri...IOSRJAC
2-oxo-2H-coumarin-3-carbohydrazide (2) which prepared from the reaction of ethyl-2-oxo-2Hcoumarin-3-carboxylate (1) with hydrazine hydrate in ethanol containing a catalytic amount of piperidine mixture consider a good and available starting intermediate for synthesis of series of functionalized coumarins. So, compound (2) was utilized as a key for the synthesis of some new (pyrazole, triazole)-2H- coumarin-2-one derivatives by the reaction with some selected reagents.
Synthesis, spectral characterization and bioactivity studies of some S-substi...Jing Zang
A new series of 5-(4-Chlorophenyl)-1,3,4-Oxadiazol-2-thiol derivatives was prepared from 4-chlorobenzoic acid (1) by converting it successively into corresponding ester (2), carbohydrazide (3) and 5-(4-Chlorophenyl)-1,3,4-Oxadiazol-2-thiol (4). Finally the target compounds, 6a-l, were synthesized by stirring 4 with different electrophiles, 5a-l, in DMF using NaH as weak base and activator. The proposed structures of newly synthesized compounds were confirmed by spectroscopic techniques such as 1H-NMR, 13C-NMR, HR-MS and EI-MS. All synthesized compounds were evaluated for their anti-bacterial, antifungal, cytotoxicity and enzyme inhibition activities. The compounds, 6e and 6g exhibited significant inhibition activity against acetyl cholinesterase enzyme (AChE) and 6j moderate activity against butyryl cholinesterase enzyme (BChE). The molecule, 4 exhibited good MIC (minimum inhibitory concentration) value against all the bacterial and fungal strains taken into account.
Study of the Electric Properties of Azo/Hydrazone Tautomeric Mixture of the ...Scientific Review SR
An azo/hydrazone mixture of the phenolic azo dye 4-(9-Anthrylazo)-1-naphthol was obtained in 58%
yield. The product was characterized using spectroscopic techniques such as IR, NMR and ms. The electric
conductivity of the tautomeric mixture was investigated in solid phase at ambient temperature. The electric
measurements revealed that the azo derivative has an electric conductivity equals 0.657 10
7
1
cm
1
and
electric resistivity of 1.521545 10
7
cm which falls within the range of the semiconductors’ electric resistivity that ranges between 10
2 and 109cm.
Synthesis, characterization and antimicrobial evaluation of novel diethyl (2-...iosrphr_editor
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
Syntheses and Characterizations of Some New N-alkyl, Isoxazole and Dioxazole ...IJAEMSJORNAL
N-alkyl and cycloadducts derivatives of 5-Chloroisatin were synthesized in good to excellent yields. The method evidences a selective N-alkylation when using 1,2-bis (2-chloroethoxy) ethane as efficient spacer at room temperature on the 5-Chloroisatin moiety. A general method for the 1,3-dipolar cycloaddition of 4-Chlorobenzaldoxime to alkynes provides a useful alternative route to get newisoxazole et dioxazole derivatives.
International Journal of Engineering Research and Applications (IJERA) is an open access online peer reviewed international journal that publishes research and review articles in the fields of Computer Science, Neural Networks, Electrical Engineering, Software Engineering, Information Technology, Mechanical Engineering, Chemical Engineering, Plastic Engineering, Food Technology, Textile Engineering, Nano Technology & science, Power Electronics, Electronics & Communication Engineering, Computational mathematics, Image processing, Civil Engineering, Structural Engineering, Environmental Engineering, VLSI Testing & Low Power VLSI Design etc.
Synthesis, characterization, in vitro cytotoxic and antioxidant activities of...ijperSS
ABSTRACT
A series of novel (Z)-3-(2-(4-(2-oxo-2H-chromen-3-yl) thiazol-2-yl-)hydrazono)indolin-2-one (8a-8d, 9) were synthesized with various substituted indole derivatives. Structures of the newly synthesized compounds were elucidated by FT-IR, 1H-NMR, 13C-NMR and API-ES Mass spectral data. The in vitro cytotoxic activities of the complexes measurement against the human cancer T-lymphocyte cell lines. In vitro evaluation of these title complexes revealed cytotoxicity from 6.8-18µg/mL against CEM, 9.2-21µg/mL against L1210, 10-19µg/mL against Molt4/C8, 8-12µg/mL against HL60 and 8-16µg/mL against BEL7402. Coumarin derivatives 8c and 8d showed that quite significant anticancer activities. The antioxidant activity of the synthesized compounds was evaluated by DPPH scavenging method. Compounds 8c, 8d and 9 showed significant antioxidant activity compared with that of standard drug, ascorbic acid.
Key words: Coumarin, DPPH, Cytotoxic activity.
A facile and efficient synthesis of some odorant Schiff bases using microwave...Pawan Kumar
Three odorant Schiff bases of methylanthranilate, an aroma constituent of blossom essential oils, with naturally occurring
odorant aldehydes- anisaldehyde, benzaldehyde and cinnamaldehyde employing microwave (MW) irradiation method were
synthesized. Elemental and spectral (FT-IR, 1H-NMR) analysis of these compounds supported their molecular structures.
Olfactory properties of these Schiff bases indicated their suitability for use in various fragrance compositions. These
compounds also showed varied antimicrobial activity against Aspergillus niger, Penicillium chrysogenum, Staphylococcus
aureus and Escherichia coli.
A facile and efficient synthesis of some odorant Schiff bases using microwave...Pawan Kumar
Three odorant Schiff bases of methylanthranilate, an aroma constituent of blossom essential oils, with naturally occurring
odorant aldehydes- anisaldehyde, benzaldehyde and cinnamaldehyde employing microwave (MW) irradiation method were
synthesized. Elemental and spectral (FT-IR, 1H-NMR) analysis of these compounds supported their molecular structures.
Olfactory properties of these Schiff bases indicated their suitability for use in various fragrance compositions. These
compounds also showed varied antimicrobial activity against Aspergillus niger, Penicillium chrysogenum, Staphylococcus
aureus and Escherichia coli.
An efficient synthesis, characterization and antibacterial activity of novel ...iosrjce
IOSR Journal of Applied Chemistry (IOSR-JAC) is a double blind peer reviewed International Journal that provides rapid publication (within a month) of articles in all areas of applied chemistry and its applications. The journal welcomes publications of high quality papers on theoretical developments and practical applications in Chemical Science. Original research papers, state-of-the-art reviews, and high quality technical notes are invited for publications.
Simple Synthesis of Some Novel Polyfunctionally Derivatives of 2H-Coumarin-2-...IOSRJAC
Compound (2) was prepared from the reaction of ethyl-2-oxo-2H-coumarin-3-carboxylate (1) with ethylcyanoacetate in ethanol containing a catalytic amount of piperidine as catalyst. Compound (2) is the key intermediate for the synthesis of several series of new compounds such as ((pyrimidine, tetrazine, piperidine, oxazepine)-2H-coumarin-2-one derivatives by reaction with selected reagents such as urea, cyanoacetamide, cyanoacetohydrazide, orthoaminophenol and 5-aminotriazole.
Oxidation of 7-Methyl Sulfanyl-5-Oxo-5H-Benzothiazolo-[3, 2-A]-Pyrimidine-6-...inventionjournals
International Journal of Engineering and Science Invention (IJESI) is an international journal intended for professionals and researchers in all fields of computer science and electronics. IJESI publishes research articles and reviews within the whole field Engineering Science and Technology, new teaching methods, assessment, validation and the impact of new technologies and it will continue to provide information on the latest trends and developments in this ever-expanding subject. The publications of papers are selected through double peer reviewed to ensure originality, relevance, and readability. The articles published in our journal can be accessed online.
Microwave Irradated Synthesis, Characterization and Evaluation for their Antibacterial and Larvicidal Activities of some Novel Chalcone and Isoxazole Substituted 9-Anilino Acridines
Similar to Synthesis, Characterization and invitro Anti- inflammatory activity of 1, 3, 4-Oxadiazole derivatives (20)
A new RP -HPLC method development and validation for simultaneous estimation ...SriramNagarajan19
A simple, accurate, precise method was developed for the simultaneous estimation of the Aspirin and Omeprazole in Tablet dosage form. Chromatogram was run through Discovery 250 x 4.6 mm, 5m. Mobile phase containing Buffer and Acetonitrile in the ratio of 70:30 v/v was pumped through column at a flow rate of 1 ml/min. Temperature was maintained at 30°C. Optimized wavelength for Aspirin and Omeprazole was 241 nm. Retention time of Aspirin and Omeprazole were found to be 2.454 min and 3.168 min %RSD of the Aspirin and Omeprazole were and found to be 1.1 and 0.8 respectively. Percentage recovery was obtained as 99.50% and 99.57%for Aspirin and Omeprazole. LOD, LOQ values were obtained from regression equations of Aspirin and Omeprazole were 0.26ppm, 0.80ppm and 0.06ppm, 0.17ppm respectively. Regression equation of Aspirin is y = 3524x + 3853, and of Omeprazole is y = 10438x+542.2.
Nutrease powder; a natural plant based nutritional shake with co-factors & co...SriramNagarajan19
Nutrease powder is an effective natural vitamin and minerals Nutritional supplementation to improve metabolism. Nutrease powder just ½ serving (1 scoop) Provides 150 calories,18 grams of protein, 12 grams of fiber, and 1 gram of sugar per day. Nutrease powder Supports effective weight management, Reduces hunger and cravings, Promotes energy and positive mood, Promotes loss of fat and preservation of lean body mass, Improves metabolism and insulin sensitivity. This article reviews the current available scientific literature regarding the effect of nutrease powder as an effective supplementation for daily energy needs.
Method development and validation of simultaneous estimation of paracetamol &...SriramNagarajan19
A drug may be defined as a substance meant for diagnosis, cure, mitigation, prevention or treatment of diseases in human beings or animals or for alternating any structure or function of the body of human being or animals. Pharmaceutical chemistry is a science that makes use of general laws of chemistry to study drugs i.e. their preparation, chemical natures, composition, structure, influence on an organism and studies the physical and chemical properties of drugs, the methods of quality control and the conditions of their storage etc. the family of drugs may be broadly classified as.
1. Pharmacodynamic agents.
2. Chemotherapeutic agents.
It is necessary to find the content of each drug either in pure or single, combined dosage forms for purity testing. It is also essential to know the concentration of the drug and it’s metabolites in biological fluids after taking the dosage form for treatment.
The scope of developing and validating analytical methods is to ensure a suitable method for a particular analyte more specific, accurate and precise. The main objective for that is to improve the conditions and parameters, which should be followed in the development and validation.
WELLIA-R tablets; helps to protect brain tissue in cerebral edemaSriramNagarajan19
Boswellia serrate extract in Wellia- R gained significant importance in treatment of cerebral edema in patients with brain tumors, colon cancer, lung cancer, blood cancer, skin cancer, breast cancer, renal cancer, fibro sarcoma, prostate cancer and pancreatic cancer. The medicinal properties of Boswellia serrate extract in Wellia- R have been known and utilized since antiquity. Its current potential as an anti inflammatory and anticancer agent are being investigated and hold great promise. This article reviews the current available scientific literature regarding the effect of wellia-R tablets, from Boswellia serrate extract that Provides long lasting cerebral protection in brain tumor patients
Formulation and invivo evaluation of mucoadhesive microspheres embedded clero...SriramNagarajan19
In this study an attempt was made to prepare mucoadhesive microcapsules of Clerodendrum phlomidis extract using alginate polymers for prolonged release. Encapsulation of extract into sodium alginate polymer was done by ionic-gelation technique. In vivo testing of the mucoadhesive microcapsules in diabetic albino rats demonstrated significant antidiabetic effect of extract. The hypoglycemic effect obtained by mucoadhesive microcapsules was for more than 16 h whereas plain CP extract produced an antidiabetic effect for only 4 h suggesting that mucoadhesive microcapsules are a valuable system for the long term delivery of CP extract. In-vivo data obtained over a 120-h period indicate that CP extract loaded alginate microspheres from batch F7 showed the better glycemic control than control and a commercial brand of the drug.
Brian stroke memory impairment and treatment strategiesSriramNagarajan19
A brain stroke occurs when one of the brain parts are deprived form oxygen-rich blood due to various mechanism. Usually a brain stroke occurs when one of the arteries is blocked either because of narrowing of small arteries with in the brain or the hardening of the arteries that lead to atherosclerosis strokes can be either ischemic (85%) or Hemorrhagic (15%). Forget fullness is a common complaint among older people. Age –related memory changes are not the same thing as dementia. Preventing memory loss is by exercise regularly staying social, manage stress, get plenty of sleep and don’t smoke. Eat plenty of fruits and vegetable and take food contain antioxidant in abundance; will reduce your risk of stroke. Walking regularly is an easy to fight memory loss and also brain exercises to prevent loss and boost brainpower. Research is going no to enhance memory power in brain in patient with brain stroke.
A new analytical method development and validation for the estimation of lenv...SriramNagarajan19
A simple and selective LC method is described for the determination of Lenvatinib dosage forms. Chromatographic separation was achieved on a c18 column using mobile phase consisting of a mixture of Phosphate buffer (KH2PO4): Acetonitrile (80:20) with detection of 240nm. Linearity was observed in the range 60-140 µg /ml for Lenvatinib (r2 =0.996) for the amount of drug estimated by the proposed methods was in good agreement with the label claim.
The proposed methods were validated. The accuracy of the methods was assessed by recovery studies at three different levels. Recovery experiments indicated the absence of interference from commonly encountered pharmaceutical additives. The method was found to be precise as indicated by the repeatability analysis, showing %RSD less than 2. All statistical data proves validity of the methods and can be used for routine analysis of pharmaceutical dosage form.
A new analytical method development and validation for the simultaneus estima...SriramNagarajan19
A simple and selective LC method is described for the determination of LEDIPASVIR and SOFOSBUVIR in tablet dosage forms. Chromatographic separation was achieved on a c18 column using mobile phase consisting of a mixture of Mixed Phosphate Buffer:ACN (55:45) with detection of 213 nm. Linearity was observed in the range 60-140 µg/ml for LEDIPASVIR oxalate (r2 =0.999) and 6-14 µg /ml for SOFOSBUVIR (r2 =0.996) for the amount of drugs estimated by the proposed methods was in good agreement with the label claim.
The proposed methods were validated. The accuracy of the methods was assessed by recovery studies at three different levels. Recovery experiments indicated the absence of interference from commonly encountered pharmaceutical additives. The method was found to be precise as indicated by the repeatability analysis, showing %RSD less than 2. All statistical data proves validity of the methods and can be used for routine analysis of pharmaceutical dosage form.
A new analytical method development and validation for the simultaneus estima...SriramNagarajan19
A simple and selective LC method is described for the determination of Ibuprofen and Tramadol in tablet dosage forms. Chromatographic separation was achieved on a c18 column using mobile phase consisting of a mixture of 60 volumes of Triethylamine buffer, 40 volumes of acetonitrile with detection of 227 nm. Linearity was observed in the range 50-150 µg/ml for Ibuprofen (r2 =0.983) and 50-150 µg /ml for Tramadol (r2 =0.985) for the amount of drugs estimated by the proposed methods was in good agreement with the label claim.
The proposed methods were validated. The accuracy of the methods was assessed by recovery studies at three different levels. Recovery experiments indicated the absence of interference from commonly encountered pharmaceutical additives. The method was found to be precise as indicated by the repeatability analysis, showing %RSD less than 2. All statistical data proves validity of the methods and can be used for routine analysis of pharmaceutical dosage form.
Method development and validation of escitalopram and estizolam in tablet dos...SriramNagarajan19
A simple and selective LC method is described for the determination of Escitalopram oxalate and Etizolam in tablet dosage forms. Chromatographic separation was achieved on a c18 column using mobile phase consisting of a mixture of 30 volumes of ammonium acetate buffer, 40 volumes of acetonitrile and 30 volumes of Methanol with detection of 238 nm. Linearity was observed in the range 60-140 µg/ml for Escitalopram oxalate (r2 =0.999) and 6-14 µg /ml for Etizolam (r2 =0.996) for the amount of drugs estimated by the proposed methods was in good agreement with the label claim.
The proposed methods were validated. The accuracy of the methods was assessed by recovery studies at three different levels. Recovery experiments indicated the absence of interference from commonly encountered pharmaceutical additives. The method was found to be precise as indicated by the repeatability analysis, showing %RSD less than 2. All statistical data proves validity of the methods and can be used for routine analysis of pharmaceutical dosage form.
Analytical method development and validation for the estimation of aspirin an...SriramNagarajan19
A simple and selective LC method is described for the determination of Aspirin and Omeprazole in tablet dosage forms. Chromatographic separation was achieved on a c18 column using mobile phase consisting of a mixture of 30 volumes of ammonium acetate buffer, 40 volumes of acetonitrile and 30 volumes of Methanol with detection of 233 nm. Linearity was observed in the range 18-42 µg/ml for Aspirin (r2 =0.983) and 6-14 µg /ml for Omeprazole (r2 =0.970) for the amount of drugs estimated by the proposed methods was in good agreement with the label claim. The proposed methods were validated. The accuracy of the methods was assessed by recovery studies at three different levels. Recovery experiments indicated the absence of interference from commonly encountered pharmaceutical additives. The method was found to be precise as indicated by the repeatability analysis, showing %RSD less than 2. All statistical data proves validity of the methods and can be used for routine analysis of pharmaceutical dosage form.
Formulation and evaluation of rosiglitazone nanosuspensionSriramNagarajan19
The main aim of this study is to formulate and evaluate Rosiglitazone Nano suspension. Nano suspensions are colloidal dispersion of Nano sized drug particles stabilized by surfactants. They can also be defined as a biphasic system consisting of pure drug particles dispersed in an aqueous vehicle in which the diameter of the suspended particle is less than 1micro meter in size. Rosiglitazone is an oral rapid and short –acting anti-diabetic drug from the sulfonylurea class. It is classified as a second generation sulfonylurea, which means that it undergoes enter hepatic circulation. Rosiglitazone Nano suspension was prepared by precipitation technique. After preparation of Nano suspension various characterization studies were done such as drug content, %yield, FTIR, DSC, TEM, and Invitro drug release.PVPK30,polaxomer are used as stabilizers. From the dissolution study F4 formulation which containts PVPK30 as stabilizer was considered as optimized formulation. It showed maximum drug release at 30min.FTIR and DSC studies revealed that good stability in dispersion.
Effect of hydrophilic polymers on solubility of some antihypertentives drugs ...SriramNagarajan19
The main aim of the present study is to carried out to enhance solubility of Felodipine. Felodipine.was selected as model drug and different carriers like Vitamin-E, Polyethylene Glycol 8000, Polyvinyl pyrrolidone K-30 were used in drug to carrier ratio 1:1, 1:2, 1:4 by weight respectively. Solid dispersions were prepared by physical mixing method and solvent evaporation method. Solid dispersions were evaluated by drug content, in-vitro release, FT-IR, DSC and XRD. The obtained data of solid dispersion prepared by solvent evaporation method were compared with physical mixing method. The result showed decrease in melting point change from crystalline to amorphous form and improved dissolution rate as compared to physical mixing as well as pure Felodipine. The finding of present study proposes that solid dispersion approach is beneficial in enhancing solubility of drug and bioavailability as well.
A review on plants act on both antidiabetic and antihyperlipidemic plantsSriramNagarajan19
Since ancient times, plants have been an exemplary source of medicine. Ayurveda and other Indian literature mentioned the use of plants in treatment of various human ailments. Medical plants play an important role in the management of diabetes mellitus especially in developing countries where resources are meager. Oral hypoglycemic agents like sulphonylureas and biguanides are still the major players in the management of the disease but there is growing interest in herbal remedies due to the side effects associated with the oral hypoglycemic agents. Herbal medicines have been the highly esteemed source of medicine throughout human history. Hyperlipidemia has been ranked as one of the greatest risk factors contributing to prevalence and severity of coronary heart diseases. Hyperlipidemia is a condition when abnormally high levels of lipids i.e. the fatty substances are found in the blood. Hypolipidemic drugs are extensively used as prophylactic agents to prevent such atherosclerosis induced disorders. But these hypolipidemic drugs are not free from adverse effects. Many plant derivatives and domestic remedies have been screened for their hypolipidemic action. More than 70 medicinal plants have been documented to have significant hypolipidemic action. During the last decade, an increase in the use of medicinal plants has been observed in metropolitan areas of developed countries. Medicinal plants play a major role in diabetes and hypolipidemic activity. The advantages of herbal medicines reported are effectiveness, safety, affordability and acceptability, this review focus on diabeties and hyperlipidemia and the role of plants used for the treatment of diabeties and hyperlipidemia.
FORMULATION AND CHARACTERISATION OF TRANSDERMAL PATCHES OF PERINDOPRILSriramNagarajan19
Transdermal drug delivery system (TDDS) has been an increased interest in the drug administration via the skin for both local therapeutic effects on diseased skin (topical delivery) as well as for systemic delivery of drugs. The skin as a site of drug delivery, has a number of significant advantages over many other routes of drug administration, including the ability to avoid problems of gastric irritation, pH and emptying rate effects, avoid hepatic first-pass metabolism thereby increasing the bioavailability of drug, reduce the risk of systemic side effects by minimizing plasma concentrations compared to oral therapy, provide a sustained release of drug at the site of application; rapid termination of therapy by removal of the device or formulation, the reduction of fluctuations in plasma levels of drugs, and avoid pain associated with injections. The transdermal delivery can also eliminate pulsed entry into the systemic circulation, which might often cause undesirable side effects. Main objective of formulating the transdermal system was to prolong the drug release time, reduce the frequency of administration and to improve patient compliance. In the present study, five formulations were prepared using single polymer in different ratios, along with plasticizers and penetration enhancer. Finally it was concluded that Some formulations show formation of brittle patch due to insufficient amount of polymer and in some patches texture of patch is not elegant due to plasticizer concentration for patch preparation. So by increasing concentration of polymer and plasticizer, finally formulation-5 was considered as optimized formula for preparing transdermal patch of Perindopril, where it shown best drug release profile.
Intercontinental journal of pharmaceutical Investigations and ResearchSriramNagarajan19
Anti-inflammatory activity of the ethanolic extract of Portulaca quadrifida Linn. was studied in wister rats using the carrageenan induced left hind paw edema, carrageenan induced pleurisy and cotton pellet induced granuloma model. The ethanolic extract (200 mg/kg, p.o.,) produced the inhibition of carrageenan induced rat paw edema. It also showed an inhibitory effect on leukocyte migration and a reduction on the pleural exudates as well as reduction on the granuloma weight in the cotton pellet granuloma method. The results indicated that the ethanolic extract produced significant (P<0.001) anti-inflammatory activity when compared with the standard and untreated control.
ANTI-BACTERIAL ACTIVITY OF EXTRACTS OF TACHYSPERMUM AMMI FRUITSSriramNagarajan19
This study was carried out with an objective to investigate the antibacterial activity of Tachyspermum ammi fruits extracts. In the present study, the anti-bacterial activity of aqueous and ethanolic extracts of Tachyspermum ammi fruits was evaluated for potential antimicrobial activity against medically important bacterial and fungal strains. The antimicrobial activity was determined using agar disc diffusion method. The antibacterial and antifungal activities of extracts were tested against Gram-positive—Staphylococcus aureus and Gram-negative—Escherichia coli human pathogenic bacteria. Zone of inhibition of extracts were compared with that of different standard drugs. The results showed that the remarkable inhibition of the bacterial growth was shown against the tested organisms. The phytochemical analyses of the plants were carried out. The antibacterial activity of the Tachyspermum ammi fruits was due to the presence of various secondary metabolites. Hence, these plants can be used to discover bioactive natural products that may serve as leads in the development of new pharmaceuticals research activities.
Live Longer, Stay healthy, Feel better with AstashinecapsulesSriramNagarajan19
ASTASHINE capsule contains natural astaxanthin from Haematococcus pluvialis Astaxanthin has exceptional antioxidant activity to combat singlet oxygen when compared to other antioxidants. In particular, Astaxanthin can be used to defend against singlet oxygen damage, which are especially susceptible to aging effects.
In this study, Astaxanthin extracted from Haematococcus microalgae powerfully quenched singlet oxygen. Results show that the quenching effect of Astaxanthin is 800 times greater than coenzyme Q10. Astaxanthin was also about 75 times greater than alpha lipoic acid, about 550 times greater than green tea catechins and about 6000 times greater than Vitamin C.the present Article reviews the role of ASTASHINE capsules as World’s most powerful Antioxidant and Anti-aging Nutrient.
Astashine capsules: an excellent choice for eye fatique relieveSriramNagarajan19
Scientists long ago discovered that a class of naturally-occurring pigments called carotenoids held powerful antioxidant properties that are crucial for eye health. This carotenoid is called astaxanthin. Astaxanthin is produced by the microalgae Haematococcus pluvialis when its water supply dries up, forcing it to protect itself from ultraviolet radiation. Astaxanthin is leaps and bounds more powerful than beta-carotene, alpha-tocopherol, lycopene, and lutein--other members of its chemical family. Astaxanthin exhibits very strong free radical scavenging activity, and protects eyes from oxidative damage. Astaxanthin is by far the most powerful carotenoid antioxidant when it comes to free radical scavenging: it is 65 times more powerful than vitamin C, 54 times more powerful than beta-carotene, and 14 times more powerful than vitamin E. Astaxanthin is far more effective than other carotenoids at "singlet oxygen quenching," which is a particular type of oxidation. The damaging effects of sunlight and various organic materials are caused by this less-stable form of oxygen. Astaxanthin is 550 times more powerful than vitamin E and 11 times more powerful than beta-carotene at neutralizing this singlet oxygen. Astaxanthin crosses the blood-brain barrier and the blood-retinal barrier which has huge implications for the health of eyes.
Anti bacterial activity of Derris indica leaf extractsSriramNagarajan19
Derris indica, family Fabaceae also known as Pongamia pinnata has various therapeutic properties. It shows activities like hepatoprotective, antirheumatic, hypoglycemic, anti bacterial etc. The plant leaves are is rich in flavanoids, alkaloids which are proved by phytochemical analysis. The aqueous, chloroform, methanolic and petroleum ether extracts were screened for anti bacterial activity using Bacillus subtilis and E. coli strain. The anti bacterial activity was performed using diffusion assay method using spread plate method. The study showed methanoilc and chloroform extracts have potent antibacterial activity. Thus Derris indica have abti bacterial activity along with other therapeutic activities.
Title: Sense of Taste
Presenter: Dr. Faiza, Assistant Professor of Physiology
Qualifications:
MBBS (Best Graduate, AIMC Lahore)
FCPS Physiology
ICMT, CHPE, DHPE (STMU)
MPH (GC University, Faisalabad)
MBA (Virtual University of Pakistan)
Learning Objectives:
Describe the structure and function of taste buds.
Describe the relationship between the taste threshold and taste index of common substances.
Explain the chemical basis and signal transduction of taste perception for each type of primary taste sensation.
Recognize different abnormalities of taste perception and their causes.
Key Topics:
Significance of Taste Sensation:
Differentiation between pleasant and harmful food
Influence on behavior
Selection of food based on metabolic needs
Receptors of Taste:
Taste buds on the tongue
Influence of sense of smell, texture of food, and pain stimulation (e.g., by pepper)
Primary and Secondary Taste Sensations:
Primary taste sensations: Sweet, Sour, Salty, Bitter, Umami
Chemical basis and signal transduction mechanisms for each taste
Taste Threshold and Index:
Taste threshold values for Sweet (sucrose), Salty (NaCl), Sour (HCl), and Bitter (Quinine)
Taste index relationship: Inversely proportional to taste threshold
Taste Blindness:
Inability to taste certain substances, particularly thiourea compounds
Example: Phenylthiocarbamide
Structure and Function of Taste Buds:
Composition: Epithelial cells, Sustentacular/Supporting cells, Taste cells, Basal cells
Features: Taste pores, Taste hairs/microvilli, and Taste nerve fibers
Location of Taste Buds:
Found in papillae of the tongue (Fungiform, Circumvallate, Foliate)
Also present on the palate, tonsillar pillars, epiglottis, and proximal esophagus
Mechanism of Taste Stimulation:
Interaction of taste substances with receptors on microvilli
Signal transduction pathways for Umami, Sweet, Bitter, Sour, and Salty tastes
Taste Sensitivity and Adaptation:
Decrease in sensitivity with age
Rapid adaptation of taste sensation
Role of Saliva in Taste:
Dissolution of tastants to reach receptors
Washing away the stimulus
Taste Preferences and Aversions:
Mechanisms behind taste preference and aversion
Influence of receptors and neural pathways
Impact of Sensory Nerve Damage:
Degeneration of taste buds if the sensory nerve fiber is cut
Abnormalities of Taste Detection:
Conditions: Ageusia, Hypogeusia, Dysgeusia (parageusia)
Causes: Nerve damage, neurological disorders, infections, poor oral hygiene, adverse drug effects, deficiencies, aging, tobacco use, altered neurotransmitter levels
Neurotransmitters and Taste Threshold:
Effects of serotonin (5-HT) and norepinephrine (NE) on taste sensitivity
Supertasters:
25% of the population with heightened sensitivity to taste, especially bitterness
Increased number of fungiform papillae
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Ve...kevinkariuki227
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
Flu Vaccine Alert in Bangalore Karnatakaaddon Scans
As flu season approaches, health officials in Bangalore, Karnataka, are urging residents to get their flu vaccinations. The seasonal flu, while common, can lead to severe health complications, particularly for vulnerable populations such as young children, the elderly, and those with underlying health conditions.
Dr. Vidisha Kumari, a leading epidemiologist in Bangalore, emphasizes the importance of getting vaccinated. "The flu vaccine is our best defense against the influenza virus. It not only protects individuals but also helps prevent the spread of the virus in our communities," he says.
This year, the flu season is expected to coincide with a potential increase in other respiratory illnesses. The Karnataka Health Department has launched an awareness campaign highlighting the significance of flu vaccinations. They have set up multiple vaccination centers across Bangalore, making it convenient for residents to receive their shots.
To encourage widespread vaccination, the government is also collaborating with local schools, workplaces, and community centers to facilitate vaccination drives. Special attention is being given to ensuring that the vaccine is accessible to all, including marginalized communities who may have limited access to healthcare.
Residents are reminded that the flu vaccine is safe and effective. Common side effects are mild and may include soreness at the injection site, mild fever, or muscle aches. These side effects are generally short-lived and far less severe than the flu itself.
Healthcare providers are also stressing the importance of continuing COVID-19 precautions. Wearing masks, practicing good hand hygiene, and maintaining social distancing are still crucial, especially in crowded places.
Protect yourself and your loved ones by getting vaccinated. Together, we can help keep Bangalore healthy and safe this flu season. For more information on vaccination centers and schedules, residents can visit the Karnataka Health Department’s official website or follow their social media pages.
Stay informed, stay safe, and get your flu shot today!
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Pulmonary Thromboembolism - etilogy, types, medical- Surgical and nursing man...VarunMahajani
Disruption of blood supply to lung alveoli due to blockage of one or more pulmonary blood vessels is called as Pulmonary thromboembolism. In this presentation we will discuss its causes, types and its management in depth.
Knee anatomy and clinical tests 2024.pdfvimalpl1234
This includes all relevant anatomy and clinical tests compiled from standard textbooks, Campbell,netter etc..It is comprehensive and best suited for orthopaedicians and orthopaedic residents.
Acute scrotum is a general term referring to an emergency condition affecting the contents or the wall of the scrotum.
There are a number of conditions that present acutely, predominantly with pain and/or swelling
A careful and detailed history and examination, and in some cases, investigations allow differentiation between these diagnoses. A prompt diagnosis is essential as the patient may require urgent surgical intervention
Testicular torsion refers to twisting of the spermatic cord, causing ischaemia of the testicle.
Testicular torsion results from inadequate fixation of the testis to the tunica vaginalis producing ischemia from reduced arterial inflow and venous outflow obstruction.
The prevalence of testicular torsion in adult patients hospitalized with acute scrotal pain is approximately 25 to 50 percent
New Drug Discovery and Development .....NEHA GUPTA
The "New Drug Discovery and Development" process involves the identification, design, testing, and manufacturing of novel pharmaceutical compounds with the aim of introducing new and improved treatments for various medical conditions. This comprehensive endeavor encompasses various stages, including target identification, preclinical studies, clinical trials, regulatory approval, and post-market surveillance. It involves multidisciplinary collaboration among scientists, researchers, clinicians, regulatory experts, and pharmaceutical companies to bring innovative therapies to market and address unmet medical needs.
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Ethanol (CH3CH2OH), or beverage alcohol, is a two-carbon alcohol
that is rapidly distributed in the body and brain. Ethanol alters many
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mortality, and public health costs than all illicit drugs combined. The
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drinking, negative social consequences, risky use, and altered physiological
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of the prevalence and harmful consequences of AUD in the U.S.,
the systemic nature of the disease, neurocircuitry and stages of AUD,
comorbidities, fetal alcohol spectrum disorders, genetic risk factors, and
pharmacotherapies for AUD.
Recomendações da OMS sobre cuidados maternos e neonatais para uma experiência pós-natal positiva.
Em consonância com os ODS – Objetivos do Desenvolvimento Sustentável e a Estratégia Global para a Saúde das Mulheres, Crianças e Adolescentes, e aplicando uma abordagem baseada nos direitos humanos, os esforços de cuidados pós-natais devem expandir-se para além da cobertura e da simples sobrevivência, de modo a incluir cuidados de qualidade.
Estas diretrizes visam melhorar a qualidade dos cuidados pós-natais essenciais e de rotina prestados às mulheres e aos recém-nascidos, com o objetivo final de melhorar a saúde e o bem-estar materno e neonatal.
Uma “experiência pós-natal positiva” é um resultado importante para todas as mulheres que dão à luz e para os seus recém-nascidos, estabelecendo as bases para a melhoria da saúde e do bem-estar a curto e longo prazo. Uma experiência pós-natal positiva é definida como aquela em que as mulheres, pessoas que gestam, os recém-nascidos, os casais, os pais, os cuidadores e as famílias recebem informação consistente, garantia e apoio de profissionais de saúde motivados; e onde um sistema de saúde flexível e com recursos reconheça as necessidades das mulheres e dos bebês e respeite o seu contexto cultural.
Estas diretrizes consolidadas apresentam algumas recomendações novas e já bem fundamentadas sobre cuidados pós-natais de rotina para mulheres e neonatos que recebem cuidados no pós-parto em unidades de saúde ou na comunidade, independentemente dos recursos disponíveis.
É fornecido um conjunto abrangente de recomendações para cuidados durante o período puerperal, com ênfase nos cuidados essenciais que todas as mulheres e recém-nascidos devem receber, e com a devida atenção à qualidade dos cuidados; isto é, a entrega e a experiência do cuidado recebido. Estas diretrizes atualizam e ampliam as recomendações da OMS de 2014 sobre cuidados pós-natais da mãe e do recém-nascido e complementam as atuais diretrizes da OMS sobre a gestão de complicações pós-natais.
O estabelecimento da amamentação e o manejo das principais intercorrências é contemplada.
Recomendamos muito.
Vamos discutir essas recomendações no nosso curso de pós-graduação em Aleitamento no Instituto Ciclos.
Esta publicação só está disponível em inglês até o momento.
Prof. Marcus Renato de Carvalho
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Synthesis, Characterization and invitro Anti- inflammatory activity of 1, 3, 4-Oxadiazole derivatives
1. ICJPIR 2014, 1(1), 5-11 Selvakumar K et al,
5
www.icjpir.com
Available online at www.icjpir.com
Intercontinental journal of pharmaceutical
Investigations and Research
ICJPIR |Volume 1 | Issue 1 | June - 2014
Research Article
Synthesis, Characterization and invitro Anti- inflammatory activity
of 1, 3, 4-Oxadiazole derivatives
*Selvakumar K1
, Joysa Ruby J1
, Rajamanickam V 2
, Jesindha Beyatricks K1
, N.Sriram3
1
Faculty of Pharmacy, Hillside College of Pharmacy and Research Centre, Bangalore-62
2
Department of Pharmaceutical Chemistry, Arulmigu Kalasalingam College of Pharmacy,
Krishnankoil, Tamilnadu, India - 626190.
3
Smt.Sarojini Rammulamma college of Pharmacy, Mahabubnagar, A.P.,India.
*Corresponding Author: K. Selvakumar, Email: kselva.pharma@gmail.com
ABSTRACT
Oxadiazole derivatives have played a vital part in the development of heterocyclic compounds. In this present work,
a series of 5-(2-aminophenyl)-1,3,4-oxadiazole-2(3H)-thione derivatives (1-10) have been synthesized by Mannich
reaction. The reaction progress of the synthesized compounds was checked by TLC. The structures of the newly
synthesized compounds were confirmed by IR and 1
H NMR spectral data. The in-vitro anti-inflammatory activity of
1, 3, 4-oxadiazole compounds (1-10) was assessed by HRBC Membrane Stabilization Method. Among the newly
synthesized 1,3,4-oxadiazole derivatives, compounds OFP, OAP, OBNP, OPBNP, ORP, OUP, OPClBP, OFD,
OAD and OBND possessed highly significant anti-inflammatory activity at a dose of 1000µg/ml when compared
with standard, Diclofenac potassium.
Keywords: 1,3,4-Oxadiazole, Mannich reaction, HRBC Membrane Stabilization Method, Anti-inflammatory,
Diclofenac potassium.
INTRODUCTION
The Oxadiazole types of heterocyclic compounds
contain oxygen and two nitrogen atoms. Various
1,3,4-oxadiazoles have been reported to have a broad
biological activities including analgesic1
, anti-
inflammatory2
, anticancer3
, anti-HIV4
, anti-
parkinson5
, antibacterial6
, antifungal7
and anti-
tubercular8
agents. These observations prompted to
synthesis 5-(2-aminophenyl)-1,3,4-oxadiazole-2(3H)-
thione and followed by a novel series of mannich
bases of 5-(2-aminophenyl)-1,3,4-oxadiazole-2(3H)-
thione.
Oxadiazole is a heterocyclic nucleus and is
considered to be derived from furan by replacement
of two methane (‐CH=) group in furan replaced by
two pyridine type nitrogen. Among the methods
employed in synthesis of 1,3,4-oxadiazole,
cyclization reaction of acid hydrazide and its
derivatives were prepared by incorporation of
secondary amines with aldehydes.
2. ICJPIR 2014, 1(1), 5-11 Selvakumar K et al,
6
www.icjpir.com
Materials and Methods
Synthesis of substituted 1,3,4-oxadiazole9
Anthranilic acid (0.01 mol) was dissolved in 20 ml
ethanol. To this, concentrated sulphuric acid was
added drop wise until the white precipitate was
formed and it was dried. Then the residue was
dissolved in ethanol and hydrazine hydrate (0.5 mol)
was added to this solution with constant shaking for
10 min. The white precipitate obtained was collected
by filtration and dissolved in ethanol. Potassium
hydroxide (0.56 mol) was added into the above
solution followed by carbon disulphide solution (0.76
mol) drop wise with constant shaking until the
formation of yellow precipitate of substituted
oxadiazole (1) and it was recrystallized from ethanol.
Synthesis of Mannich base substituted 1,3,4-
oxadiazoles 9
Equimolar quantities (0.01mol) of substituted
oxadiazole and respective compounds containing
secondary amine such as N-(4-hydroxyphenyl)
acetamide, N-(2,3-xylyl) anthranilic acid and
potassium 2-(2-(2,6-dichloro anilino) phenyl) acetate
were dissolved in ethanol (30 ml). To the above
mixture, the corresponding aldehyde (0.01mol) such
as formaldehyde and acetaldehyde was added and
reflux for 3-5 h. The content was kept overnight in
the freezer. The respective compound obtained was
recrystallised from ethanol.
Melting point was determined on electrical melting
point apparatus by open-ended capillary tube. The
purity of the compounds were checked by TLC using
Silica Gel as stationary phase and chloroform-
methanol (8:2) as eluent and the spots were visually
detected in an Iodine chamber10
. The structure of the
synthesized compounds was elucidated by IR spectra
in υmax (cm-1
) on FT-IR (Shizmadu-8400 series)
using KBr disc technique 11,12
and 1
H NMR spectra in
δ units (ppm) relative to an internal standard of
tetramethylsilane on 1
H NMR (Brucker 400 MHz) in
DMSO-d6 13
. The synthetic method is depicted
below.
5-(2-aminophenyl)-1,3,4-oxadiazole-2(3H)-thione
3. ICJPIR 2014, 1(1), 5-11 Selvakumar K et al,
7
www.icjpir.com
C8H7N3OS; Yield: 85.5%; mp: 155-1570
C; Rf: 0.45;
IR (KBr,υmax cm-1
): 3482.24 (NH2 ), 3154 (NH),
1624.32 (N –N), 1224.21 (C=S), 1224.21 (C=S); 1
H
NMR (δ ppm): 3.8 (s,NH2, 2H), 6.0 (s, NH, 1H), 6.6
– 7.8 (m, ArH, 4H).
N-((5-(2-aminophenyl)-2-thioxo-1,3,4-oxadiazol-
3(2H)-yl)methyl)-N-(4-hydroxyphenyl) acetamide
C17H16N4O3S; Yield: 71.78%; mp: 178-180o
C; Rf
0.581.IR (KBr, υmax cm-1
): 3426 (OH), 3343 (NH2),
1651 (N –N),1457(CH3), 1426 (CH2) 1120 (C=S); 1
H
NMR (δ ppm): 2.2(s,3H, CH3), 3.5 (s, 2H, NH2),
4.7(s, 2H, CH2), 6.6 – 7.4 (m,8H, ArH), 9.8 (s, 1H,
OH).
N-(1-(5-(2-aminophenyl)-2-thioxo-1,3,4-oxadiazol-
3(2H)-yl)ethyl)-N-(4-hydroxyphenyl) acetamide
C18H18N4O3S; Yield: 70.76%; m.p.198-200o
C; Rf
0.641. IR (KBr, υmax cm-1
): 3386 (OH), 3286 (NH2),
2084 (CH),1605(N-N), 1454 (CH3), 1422 (CH2),
1122 (C=S); 1
H NMR (δppm): 1.28 (d, 3H, CH3),
1.98 (s, 3H, CH3), 3.42 (s, 2H,NH2), 4.64(q, 1H, CH),
6.46 – 7.44 (m, 8H, ArH), 9.62 (s,1H, OH).
Potassium-2-(2-(((5-(2-aminophenyl)-2-thioxo-
1,3,4-oxadiazol-3(2H)-yl)methyl)(2,6-dichloro
phenyl) amino)phenyl) acetate
C23H17N4O3SCl2K; Yield: 69.19%; m.p. 210-212o
C;
Rf 0.612.IR (KBr, υmax cm-1
): 3257 (NH2), 1650
(C=O), 1615 (N-N),1436(CH2), 1120( C=S); 1H
NMR (δ ppm) : 1
H NMR (δppm): 3.44 (s, 2H, CH2),
4.62 (s, 2H, CH), 4.26 (s, 2H, NH2),6.52 – 7.48 (m,
11H, ArH).
Potassium-2-(2-((1-(5-(2-aminophenyl)-2-thioxo-
1,3,4-oxadiazol-3(2H)-yl)ethyl)(2,6-dichloro
phenyl) amino)phenyl) acetate
C24H19N4O3SCl2K; Yield: 59.18%; m.p. 186-188o
C;
Rf 0.812.IR (KBr, υmax cm-1
): 3272 (NH2), 1649
(C=O), 1622 (N-N),1456 (CH3), 1449 (CH2),
1121(C=S); 1
H NMR (δ ppm): 1.26(d, 3H, CH3),
3.52 (s, 2H, CH2), 3.98 (q, 1H, CH), 4.12 (s,
2H,NH2), 6.36 – 7.24 (m, 11H, ArH), 9.62 (s, 1H,
OH).
2-(((5-(2-aminophenyl)-2-thioxo-1,3,4-oxadiazol-
3(2H)-yl)methyl)(2,3-dimethylphenyl) amino
benzoic acid
C24H22N4O3S; Yield: 68.70 %; m.p 254-256o
C; Rf
0.840. IR (KBr, υmax cm-1
):.3335(OH), 3226(NH2),
1675(C=O), 1615 (N-N), 1459 (CH3), 1439 (CH2),
1190 (C=S); 1
H NMR(δ ppm) : 2.28 (s, 3H, CH3),
4.46(s, 2H, CH2), 3.82 (s, 2H,NH2), 6.16 – 7.64 (m,
11H, ArH), 10.46 (br, 1H, OH).
2-((1-(5-(2-aminophenyl)-2-thioxo-1,3,4-oxadiazol-
3(2H)-yl)ethyl)(2,3-dimethylphenyl) amino)
benzoic acid
C25H24N4O3S; Yield: 70.76 %; m.p. 244-246o
C; Rf
0.770. IR(KBr, υmax cm-1
):. 3343 (OH), 3286 (NH2),
1650 (C=O),1628 (N-N), 1449 (CH3), 1428 (CH2),
1123 (C=S); 1
H NMR (δppm) 1.24 (d, 3H, CH3), 2.26
(s, 3H, CH3), 3.72 (s, 2H,NH2), 6.08 – 8.24 (m, 11H,
ArH), 10.64 (br, 1H, OH).
PHARMACOLOGICAL STUDIES
The In-Vitro Anti-Inflammatory Effect of Novel
Oxadiazole Derivatives By HRBC Membrane
Stabilisation Method14, 15, 16
Inflammation is a tissue-reaction to infection,
irritation or foreign substance. It is a part of the host
defense mechanism but when it becomes great it is
hopeless condition. Aging is also considered to be an
inflammatory response. There are several tissue
factors or mechanisms that are known to be involved
in the inflammatory reactions such as release of
histamine, bradykinin and prostaglandins. The
development of non-steroidal anti-inflammatory
agents in recent years have contributed a lot in not
only overcoming the human sufferings such as
arthiritis but also has helped in understanding the
tissue mechanism of action of anti-inflammatory
drugs. The synthesized compounds were used for this
study. They were made into doses of 1000µg/ml with
1% acacia solution. Diclofenac sodium is taken as
standard.
The reaction mixtures (4.5ml) consisted of 2ml of
hypotonic saline (0.25% NaCl), 1ml of 0.15 M
phosphate buffer (pH 7.4, 0.15 M), and 1ml of test
solution (1000µg /ml) in normal saline. 0.5 ml of
10% HRBC in normal saline was added. For control
tests, 1ml of isotonic saline was used instead of test
solution while product control tests lacked red blood
cells. The mixtures were incubated at 560
C for 30
minutes. Then they were cooled under running tap
water and centrifuged at 3000rpm for 20 minutes.
4. ICJPIR 2014, 1(1), 5-11 Selvakumar K et al,
8
www.icjpir.com
The absorbance of the supernatants was read at
560nm. Percentage membrane stabilizing activity
was calculated as follows.
Percentage stabilization = 100- (OD of sample-OD of product control) x 100
OD of test control
The control represents 100% lysis.
HRBC Membrane Stabilization Method15, 16
:
Alseviers Solution: 2gm dextrose + 0.8gm sodium citrate + 0.05gm
Citric acid + 0.42gm sodium chloride
Make up with distilled water to 100ml
0.5ml OF 10% HRBC Suspension: 3ml of blood + 3ml of Alseviers solution
Centrifuge at 3000 rpm for 20 minutes
Packed cells were washed with isotonic saline
10% v/v Suspension of the packed cells was made with isotonic saline.
Hypotonic Saline: 0.36 gm of sodium chloride in 100ml of distilled water.
Isotonic Saline: 0.85gm of sodium chloride in 100ml of distilled water.
Phosphate Buffer (pH 7.4, 0.15 M): 2.38gm of disodium hydrogen phosphate +
0.19gm of potassium dihydrogen phosphate + 8gm of sodium chloride
Make up with 100ml of distilled water
5. ICJPIR 2014, 1(1), 5-11 Selvakumar K et al,
9
www.icjpir.com
Table 1 In Vitro ANTI INFLAMMATORY ACTIVITY OF TITLED COMPOUNDS
S.No Treatment Percentage Stabilization
(Mean ± SEM)
1. OFP 72.50 ± 0.9400**
2. OAP 65.16 ± 0.5416**
3. OBNP 71.50 ± 0.8146**
4. OPBNP 71.16 ± 0.5416**
5. ORP 62.30 ± 0.9583**
6. OUP 62.66 ± 0.9166**
7. OPClBP 63.78 ± 0.5426**
8. OFD 44.80 ± 0.9400**
9. OAD 62.30 ± 0.6666**
10. OBND 52.40 ± 0.7812**
Control 4.3262 ± 0.6780
Standard 84.50 ± 0.5000**
P < 0.001 indicates the significant difference compared with control
** Highly significant
BIO STATISTICAL ANALYSIS
All the data (Mean ± SEM) were evaluated by
student’s “t” test17, 18
and the probability was
determined for all the newly synthesized compounds
and the results were tabulated in the following Table.
1
0
10
20
30
40
50
60
70
80
PercentageStabilization
Control
Standard
OFP
OAP
OBNP
OPBNP
ORP
OUP
OPClBP
OFD
OAD
OBND
Treatment (1000mcg/ml)
In-vitro Anti-inflammatory Activity of
Titled Compounds
6. ICJPIR 2014, 1(1), 5-11 Selvakumar K et al,
10
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RESULTS AND DISCUSSION
The substituted oxadiazole, 5-(2-aminophenyl)-1,3,4-
oxadiazole-2(3H)-thione was synthesized by reacting
anthranilic acid with ethanol in presence of sulphuric
acid followed by reacting with hydrazine hydrate,
carbon disulphide and alkali. The titled oxadiazole
derivatives were synthesized by making substitution
at free N-(3H) position of substituted oxadiazole, 5-
(2-aminophenyl)-1,3,4-oxadiazole-2(3H)-thione
through Mannich condensation with secondary
amine bearing compounds such as N-(4-
hydroxyphenyl) acetamide, N-(2,3-xylyl) anthranilic
acid, potassium 2-(2-(2,6-dichloro anilino) phenyl)
acetate and series of aldehydes like formaldehyde,
acetaldehyde. The synthesized compounds were
characterized by various methods such as melting
point, IR Spectroscopy, NMR spectroscopy. The
compounds purity was further established by
chromatographic method (TLC).
In-Vitro Anti-Inflammatory Activity:
Among these synthesized compounds, compounds
OFP, OAP, OBNP, OPBNP, ORP, OUP, OPClBP,
OFD, OAD and OBND were screened for in-vitro
anti-inflammatory activity by HRBC Membrane
Stabilization Method at a concentration of
1000µg/ml. All the above evaluated compounds
possessed highly significant anti-inflammatory
activity at a dose of 1000 µg/ml when compared with
standard, Diclofenac potassium 1000µg/ml.
CONCLUSION
The titled oxadiazole derivatives were synthesized by
making substitution at free N-(3H) position of 5-(2-
aminophenyl)-1,3,4-oxadiazole-2(3H)-thione through
Mannich condensation. All the evaluated compounds
possessed highly significant anti-inflammatory
activity at a dose of 1000µg/ml when compared with
standard, Diclofenac potassium 1000µg/ml.
ACKNOWLEDGEMENTS
The authors are thankful to everyone who rendered
us support throughout and made this study
successful.
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