Design, synthesis, characterization and biological evaluation of 3- (4-(7-chloro-2-(4-chlorophenyl)-4-oxo-quinazolin-3(4H)- yl)phenyl)-2-aryl 1,3-thiazolidin-4-ones as a new class of antimicrobial agents
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.
Synthesis, Characterization, and Antifungal Evaluation of Some New 1,3,5-Tris...BRNSS Publication Hub
Objective: The objective of the paper was to design, synthesis, and characterization of new 1,3,5-trisubstituted-2-pyrazolines derivative and evaluate for antifungal activity. Materials and Methods: The 1,3,5-tri-substituted-2-pyrazolines derivatives have been synthesized by the reaction of chalcone derivatives with succinic hydrazide in the environment of pyridine. Total 20 compounds have been synthesized and characterized by the IR, 1H NMR, and mass spectral analysis. Antifungal activity of the compounds carried out on four fungal strains, that is, Saccharomyces cerevisiae, Aspergillus niger, Candida albicans, and Rhizopus oryzae in two different concentrations, that is, 50 and 100 μg/ml by agar-diffusion method using cup-plate method and Ketoconazole was used as standard antifungal drug. Results and Discussion: In accordance with the data from antifungal activity, all the synthesized 1,3,5-trisubstituted pyrazole derivatives (ME1-ME8, CL1-CL8, and BR1-BR4) have shown mild to best activity against tested organisms. The data of antifungal activity against the fungal strains (S. cerevisiae, A. niger, C. albicans, and R. oryzae) suggested the order of activity of compounds: BR-3 > BR-2 > BR-1 > CL-4 > BR-4 > CL-3 > CL-2 > ME-3> ME-2 > CL-5 > CL-6 > ME-4 > ME-5 > ME-6 > ME-7 > CL-7 > CL-8 > ME-8 > CL-1 > ME-1. The presence of electronegative group (Br, Cl, F, and NO2) either at third and fifth position of 1,3,5-pyrazoline ring is required for the potent antifungal activity. The presence of electronegative group (Br, Cl) at third and fifth position may necessary for the best activity against bacterial and fungal strains but the addition of F, NO2 has shown the moderate activity but in case of -CH3 and -OCH3 substitution may diminish the activity. The series BR-1 to BR-4 is most active compound of the synthesized compounds. Conclusion: The 1,3,5-trisubstituted pyrazole derivatives has been successfully synthesized and antifungal activity of the compounds denotes that the series BR-1 to BR-4 is most active compound of the all twenty synthesized compounds. The addition of electronegative group (Br, Cl) at third and fifth position in pyrazole ring may necessary for the activity against fungal strains.
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 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
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).
Synthesis, Characterization, and Antifungal Evaluation of Some New 1,3,5-Tris...BRNSS Publication Hub
Objective: The objective of the paper was to design, synthesis, and characterization of new 1,3,5-trisubstituted-2-pyrazolines derivative and evaluate for antifungal activity. Materials and Methods: The 1,3,5-tri-substituted-2-pyrazolines derivatives have been synthesized by the reaction of chalcone derivatives with succinic hydrazide in the environment of pyridine. Total 20 compounds have been synthesized and characterized by the IR, 1H NMR, and mass spectral analysis. Antifungal activity of the compounds carried out on four fungal strains, that is, Saccharomyces cerevisiae, Aspergillus niger, Candida albicans, and Rhizopus oryzae in two different concentrations, that is, 50 and 100 μg/ml by agar-diffusion method using cup-plate method and Ketoconazole was used as standard antifungal drug. Results and Discussion: In accordance with the data from antifungal activity, all the synthesized 1,3,5-trisubstituted pyrazole derivatives (ME1-ME8, CL1-CL8, and BR1-BR4) have shown mild to best activity against tested organisms. The data of antifungal activity against the fungal strains (S. cerevisiae, A. niger, C. albicans, and R. oryzae) suggested the order of activity of compounds: BR-3 > BR-2 > BR-1 > CL-4 > BR-4 > CL-3 > CL-2 > ME-3> ME-2 > CL-5 > CL-6 > ME-4 > ME-5 > ME-6 > ME-7 > CL-7 > CL-8 > ME-8 > CL-1 > ME-1. The presence of electronegative group (Br, Cl, F, and NO2) either at third and fifth position of 1,3,5-pyrazoline ring is required for the potent antifungal activity. The presence of electronegative group (Br, Cl) at third and fifth position may necessary for the best activity against bacterial and fungal strains but the addition of F, NO2 has shown the moderate activity but in case of -CH3 and -OCH3 substitution may diminish the activity. The series BR-1 to BR-4 is most active compound of the synthesized compounds. Conclusion: The 1,3,5-trisubstituted pyrazole derivatives has been successfully synthesized and antifungal activity of the compounds denotes that the series BR-1 to BR-4 is most active compound of the all twenty synthesized compounds. The addition of electronegative group (Br, Cl) at third and fifth position in pyrazole ring may necessary for the activity against fungal strains.
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 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
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).
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 Application of Direct Dyes Derived From Terephthalic and Isopht...IOSR Journals
Abstract: The synthesis of direct dyes derived from terephthalic and isophthalic acid using J and H- acids was
undertaken with the view of replacing benzidine moiety in the production of direct dyes. The amide derivatives
of isophthalic and terephthalic acids were used as the coupling components while aniline and its derivatives
were used as the source of diazo components. The amide derivatives were characterized by Gas
Chromatography/Mass Spectrometry and Infra-red analysis. The spectroscopic properties of the dyes in various
solvents were also examined and most of the dyes showed bathochromic shifts when the solvent was changed to
more polar solvents. The dyes also showed positive and negative halochromism with the addition of few drops of
hydrochloric acid (HCl). The synthesized dyes were applied to cotton fabrics and their performance properties
evaluated. They have good exhaustion in the presence of electrolyte and have good wash fastness properties
upon application of after-treating agents of values of 3-4, 4 and 4-5. They also had good fastness properties to
light of values between 4-7. Their resistance to rubbing and perspiration had values between 3 and 4-5. The
toxicity of the synthesized coupling components was studied using the Dietrich Lorke (LD50) method on Albino
miceand they were found to be non-toxic.
Key words: Benzidine, direct dyes, exhaustion, electrolyte, cotton, fastness.
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.
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.
This is an Engg Biotechnology project based on medicinal plant i.e singapore cherry or jamaican cherry tree (scientific name Muntingia calabure ), we did in 2013 in GMIT college Davangere, karanataka, India. i have complete project detail what we did..,
STUDIES ON TREATMENT OF PHARMACEUTICAL WASTE EFFLUENTS BY POLYMER MATERIALS M...EDITOR IJCRCPS
In the present study, sorption technique was used to achieve the optimum recovery of the pharmaceutical waste from effluents.
The modified urea formaldehyde resin was prepared and mixed with inorganic adsorbent at various proportions. The removal
capabilities of pharmaceutical waste by the prepared composite materials were investigated. Different factors affecting the uptake
such as contact time, pH value and aqueous volume to resin weight ratio have been investigated. The reaction mechanisms and
the optimum conditions for the treatment were deduced in the light of the obtained results.
Keywords: Sorption technique, Pharmaceutical waste, Different factors.
Synthesis And Antibacterial Activity Of 3-[(3-Phenyl-5-Thioxo-1, 5-Dihydro-4h...inventionjournals
A series of 3-[(3-phenyl-5-thioxo-1,5-dihydro-4H-1,2,4-triazol-4-yl)imino]-1,3-dihydro-2Hindole-2-one derivatives were synthesised through the nucleophilic substitution at carbonyl carbon of Isatin. Structure of synthesized compounds were elucidated by using IR, 1H NMR & 13C NMR spectrometry. Synthesised compounds showed significant antibacterial activity against E.coli (ATCC 35218), S.aureus (ATCC 25323), E.faecalis (Clinical isolate), K. Pneumonia, P. aeruginosa (ATCC 27893) using agar well diffusion method.
Synthesis and Pharmacological Evaluation of Novel Heterocyclic CompoundIJSRD
2-[(4-bromo anilino)]-4-chloro-6-morpholino-1,3,5-triazine[2a] and 4-chloro-N-(4-fluorophenyl)-6-morpholino-1,3,5-triazin-2-amine [2b]were synthesized and studied for their biological activity. These compounds were prepared by the condensation of 4-bromoaniline and 4-fluoroaniline with 4-(4,6-dichloro-1,3,5-triazin-2-yl) morpholine [1] which is prepared by the reaction between 2,4,6-trichloro-1,3,5-triazine and morpholine. All the compounds were characterized by elemental analysis and spectral studies.
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).
All manuscripts are subject to rapid peer review. Those of high quality (not previously published and not under consideration for publication in another journal) will be published without delay.
Ntioxidant study of usnic acid and its derivative usnic acid diacetateeSAT Journals
Abstract
Currently interest towards the study of antioxidant efficiency of the lichen metabolites was given prior attention in the field of research. As the free radical accumulation in human cells causes several chronic diseases which can be eliminated with the help of antioxidants. In our present study we have isolated the lichen secondary metabolite Usnic acid from Usnea luridorufa and also prepared the acetyl derivative of Usnic acid. The in vitro antioxidant activity of Usnic acid and Usnic acid diacetate under DPPH free radical scavenging, FRAP, Superoxide dismutase activity, Metal chelating activity, Phosphomolybdenum activity, Hydroxyl scavenging activity, Lipid peroxidation inhibiting activity were studied. The antioxidant potential of the Usnic acid and its derivative Usnic acid diacetate were compared. The IC50 value are also determined. Both the test compounds possesses significant antioxidant activity under the studies.
Keywords: Antioxidant efficiency, Usnic acid, diacetate, Tannic acid.
Evaluation of the Antioxidant Activities of Organic Extracts from Ammodaucus ...CrimsonAlternativemedicine
Aromatic and medicinal plants are a good source of natural preparations containing effective bioactive compounds which can be used for different applications. This work aims to evaluate the antioxidant activity of some organic extracts of Ammodaucus leucotrichus Coss & Dur fruit part. The whole plant was collected from the region of Beni Abbas (Bechar-Algeria). Five organic extracts were obtained and the evaluation of the antioxidant activity was performed by six conventional methods. Polar organic extracts exhibited more antioxidant power then non polar extracts. The level of phenolic compounds was moderate in all extracts. The investigation of the antioxidant activity of organic extracts from fruit part of Ammodaucus leucotrichusrevealed a moderate activity tested by six conventional methods.
For more open access journals in Crimson Publishers please click on link: https://crimsonpublishers.com/
For more articles in open access Complementary Medicine journals please click on link: https://crimsonpublishers.com/acam/
Synthesis, Characterization and Antiinflammatory activity of Cinnolines (pyra...iosrjce
IOSR Journal of Pharmacy and Biological Sciences(IOSR-JPBS) is a double blind peer reviewed International Journal that provides rapid publication (within a month) of articles in all areas of Pharmacy and Biological Science. The journal welcomes publications of high quality papers on theoretical developments and practical applications in Pharmacy and Biological Science. Original research papers, state-of-the-art reviews, and high quality technical notes are invited for publications.
Evaluation of antioxidant and antiradical properties of pomegranate (punica g...Pritam Kolge
Evaluation of antioxidant and antiradical properties
of Pomegranate (Punica granatum L.) seed and defatted
seed extracts
This is Journal Club activity Presentation with the reference of various research papers.
This Presentation Contain following...
#Info about Paper
#Abstract
#Materials
#Methods
#Results
#Discussion
#Conclusion
#References
*Important Methods used
#Moisture content
#Fat content
#Acid value
#Peroxide value
#Oxidative stability index
#Total phenols content
#Preparation of Pomegranate seed extracts and calculate extract yield
#Evaluation of antioxidant properties of Pomegranate seed extracts using
-DPPH radicals scavenging activity
-FRAP assay
#Antioxidant efficiency of seed extract (Oxidative stability extract)
#Statistical analysis
Journal Club Presentation at Bharati Vidyapeeth College of Pharmacy, Kolhapur.
Thanks for Help and Guidance of Dr. P. B. Choudhari (Assistant Professor, Pharmaceutical Chemistry) and Dr. A. J. Shinde (Assistant Professor, Department of Pharmaceutics)
Qualitative Evaluation and Wound Healing Potential of Selected Medicinal Plan...BRNSS Publication Hub
Objective: The aim of the paper was to assess the wound healing potential of three medicinal plants using the excision wound healing model on albino rat. Materials and Methods: Soxhlet extraction method was utilized for the partition of the constituent of interest. Qualitative analysis and phytochemical screening were performed for the detection of tannins, alkaloids, resins, flavonoids, glycosides, steroids, proteins, carbohydrates, and amino acids. Three plants extract used for the ointment formulation and prepared by the addition of extract of Artocarpus heterophyllus, Murraya koenigii, and Punica granatum in polyethylene glycol ointment base. Three ointment formulations and six extracts with 5% and 10% extract concentration have been used. Excision wound rat model utilized for the wound healing potential. Results and Conclusion: All three plants, including A. heterophyllus Lam., M. koenigii Linn., and P. granatum Linn. extracted for the active constituent. The pharmacological evaluation on the excision wound healing model suggested that Group-I animals showed 52.09% of healing, whereas povidone-iodine treated animals showed 100.00% healing. On the other hand, the ointment formulation treated F-1 showed 96.47% of wound healing, F-2 showed 97.68% healing, and F-3 showed 99.11% healing. The overall healing results can be represented as following: Control <MKL5 <MKL10 <PGB5 <PGB10 <AHP5 <AHP10 <F-1 <F-2 <F-3 <Standard. F3 ointment formulation is better than the F2 and F1 formulation in wound healing potential as compared to others. Discussion: These studies have indicated that ointment formulations of A. heterophyllus, M. koenigii, P. granatum have been utilized for wound healing potential and it is safer for topical application. Excision wound healing model suggested that the three individual plant extract has shown the wound healing potential, although the prepared ointment formulations F3 have best and synergistic action than the individual. The ointment formulations containing plant extracts in 10% amount have better wound healing potential.
Synthesis, Characterization and Biological Evaluation of Oxazolone Derivativesijceronline
A series of six 4-aryl Benzelidene-2-phenyl-5- oxazolone derivatives were synthesized by condensation of aromatic aldehydes with N-benzoyl glycine (Hippuric acid) in the presence of sodium acetate and acetic anhydride at room temperature in ethanol. Six of the compounds are new derivatives. The structures of the compounds were evaluated based on 1H-NMR , IR and FTIR methods and by elemental analysis. .All the derivative compounds prepared were tested for their antimicrobial activity by disk diffusion technique. Test organisms: Bacteria like Staphylococcus aureusMTCC 7443 and Salmonella typhimuriumMTCC 733 Fungi like C.albicans and A.flavus The results were compared with those of the standard 0.5% Ciprofloxacin. The derivatives with Salicylaldehyde and cinnamaldehyde were showed excellent activities against E. coli. and Staphylococcus aureusMTCC 7443 : than Salmonella typhimuriumMTCC 733 bacteria. It also showed reasonable activity withFungi like C.albicans than A.flavus
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 Application of Direct Dyes Derived From Terephthalic and Isopht...IOSR Journals
Abstract: The synthesis of direct dyes derived from terephthalic and isophthalic acid using J and H- acids was
undertaken with the view of replacing benzidine moiety in the production of direct dyes. The amide derivatives
of isophthalic and terephthalic acids were used as the coupling components while aniline and its derivatives
were used as the source of diazo components. The amide derivatives were characterized by Gas
Chromatography/Mass Spectrometry and Infra-red analysis. The spectroscopic properties of the dyes in various
solvents were also examined and most of the dyes showed bathochromic shifts when the solvent was changed to
more polar solvents. The dyes also showed positive and negative halochromism with the addition of few drops of
hydrochloric acid (HCl). The synthesized dyes were applied to cotton fabrics and their performance properties
evaluated. They have good exhaustion in the presence of electrolyte and have good wash fastness properties
upon application of after-treating agents of values of 3-4, 4 and 4-5. They also had good fastness properties to
light of values between 4-7. Their resistance to rubbing and perspiration had values between 3 and 4-5. The
toxicity of the synthesized coupling components was studied using the Dietrich Lorke (LD50) method on Albino
miceand they were found to be non-toxic.
Key words: Benzidine, direct dyes, exhaustion, electrolyte, cotton, fastness.
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.
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.
This is an Engg Biotechnology project based on medicinal plant i.e singapore cherry or jamaican cherry tree (scientific name Muntingia calabure ), we did in 2013 in GMIT college Davangere, karanataka, India. i have complete project detail what we did..,
STUDIES ON TREATMENT OF PHARMACEUTICAL WASTE EFFLUENTS BY POLYMER MATERIALS M...EDITOR IJCRCPS
In the present study, sorption technique was used to achieve the optimum recovery of the pharmaceutical waste from effluents.
The modified urea formaldehyde resin was prepared and mixed with inorganic adsorbent at various proportions. The removal
capabilities of pharmaceutical waste by the prepared composite materials were investigated. Different factors affecting the uptake
such as contact time, pH value and aqueous volume to resin weight ratio have been investigated. The reaction mechanisms and
the optimum conditions for the treatment were deduced in the light of the obtained results.
Keywords: Sorption technique, Pharmaceutical waste, Different factors.
Synthesis And Antibacterial Activity Of 3-[(3-Phenyl-5-Thioxo-1, 5-Dihydro-4h...inventionjournals
A series of 3-[(3-phenyl-5-thioxo-1,5-dihydro-4H-1,2,4-triazol-4-yl)imino]-1,3-dihydro-2Hindole-2-one derivatives were synthesised through the nucleophilic substitution at carbonyl carbon of Isatin. Structure of synthesized compounds were elucidated by using IR, 1H NMR & 13C NMR spectrometry. Synthesised compounds showed significant antibacterial activity against E.coli (ATCC 35218), S.aureus (ATCC 25323), E.faecalis (Clinical isolate), K. Pneumonia, P. aeruginosa (ATCC 27893) using agar well diffusion method.
Synthesis and Pharmacological Evaluation of Novel Heterocyclic CompoundIJSRD
2-[(4-bromo anilino)]-4-chloro-6-morpholino-1,3,5-triazine[2a] and 4-chloro-N-(4-fluorophenyl)-6-morpholino-1,3,5-triazin-2-amine [2b]were synthesized and studied for their biological activity. These compounds were prepared by the condensation of 4-bromoaniline and 4-fluoroaniline with 4-(4,6-dichloro-1,3,5-triazin-2-yl) morpholine [1] which is prepared by the reaction between 2,4,6-trichloro-1,3,5-triazine and morpholine. All the compounds were characterized by elemental analysis and spectral studies.
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).
All manuscripts are subject to rapid peer review. Those of high quality (not previously published and not under consideration for publication in another journal) will be published without delay.
Ntioxidant study of usnic acid and its derivative usnic acid diacetateeSAT Journals
Abstract
Currently interest towards the study of antioxidant efficiency of the lichen metabolites was given prior attention in the field of research. As the free radical accumulation in human cells causes several chronic diseases which can be eliminated with the help of antioxidants. In our present study we have isolated the lichen secondary metabolite Usnic acid from Usnea luridorufa and also prepared the acetyl derivative of Usnic acid. The in vitro antioxidant activity of Usnic acid and Usnic acid diacetate under DPPH free radical scavenging, FRAP, Superoxide dismutase activity, Metal chelating activity, Phosphomolybdenum activity, Hydroxyl scavenging activity, Lipid peroxidation inhibiting activity were studied. The antioxidant potential of the Usnic acid and its derivative Usnic acid diacetate were compared. The IC50 value are also determined. Both the test compounds possesses significant antioxidant activity under the studies.
Keywords: Antioxidant efficiency, Usnic acid, diacetate, Tannic acid.
Evaluation of the Antioxidant Activities of Organic Extracts from Ammodaucus ...CrimsonAlternativemedicine
Aromatic and medicinal plants are a good source of natural preparations containing effective bioactive compounds which can be used for different applications. This work aims to evaluate the antioxidant activity of some organic extracts of Ammodaucus leucotrichus Coss & Dur fruit part. The whole plant was collected from the region of Beni Abbas (Bechar-Algeria). Five organic extracts were obtained and the evaluation of the antioxidant activity was performed by six conventional methods. Polar organic extracts exhibited more antioxidant power then non polar extracts. The level of phenolic compounds was moderate in all extracts. The investigation of the antioxidant activity of organic extracts from fruit part of Ammodaucus leucotrichusrevealed a moderate activity tested by six conventional methods.
For more open access journals in Crimson Publishers please click on link: https://crimsonpublishers.com/
For more articles in open access Complementary Medicine journals please click on link: https://crimsonpublishers.com/acam/
Synthesis, Characterization and Antiinflammatory activity of Cinnolines (pyra...iosrjce
IOSR Journal of Pharmacy and Biological Sciences(IOSR-JPBS) is a double blind peer reviewed International Journal that provides rapid publication (within a month) of articles in all areas of Pharmacy and Biological Science. The journal welcomes publications of high quality papers on theoretical developments and practical applications in Pharmacy and Biological Science. Original research papers, state-of-the-art reviews, and high quality technical notes are invited for publications.
Evaluation of antioxidant and antiradical properties of pomegranate (punica g...Pritam Kolge
Evaluation of antioxidant and antiradical properties
of Pomegranate (Punica granatum L.) seed and defatted
seed extracts
This is Journal Club activity Presentation with the reference of various research papers.
This Presentation Contain following...
#Info about Paper
#Abstract
#Materials
#Methods
#Results
#Discussion
#Conclusion
#References
*Important Methods used
#Moisture content
#Fat content
#Acid value
#Peroxide value
#Oxidative stability index
#Total phenols content
#Preparation of Pomegranate seed extracts and calculate extract yield
#Evaluation of antioxidant properties of Pomegranate seed extracts using
-DPPH radicals scavenging activity
-FRAP assay
#Antioxidant efficiency of seed extract (Oxidative stability extract)
#Statistical analysis
Journal Club Presentation at Bharati Vidyapeeth College of Pharmacy, Kolhapur.
Thanks for Help and Guidance of Dr. P. B. Choudhari (Assistant Professor, Pharmaceutical Chemistry) and Dr. A. J. Shinde (Assistant Professor, Department of Pharmaceutics)
Qualitative Evaluation and Wound Healing Potential of Selected Medicinal Plan...BRNSS Publication Hub
Objective: The aim of the paper was to assess the wound healing potential of three medicinal plants using the excision wound healing model on albino rat. Materials and Methods: Soxhlet extraction method was utilized for the partition of the constituent of interest. Qualitative analysis and phytochemical screening were performed for the detection of tannins, alkaloids, resins, flavonoids, glycosides, steroids, proteins, carbohydrates, and amino acids. Three plants extract used for the ointment formulation and prepared by the addition of extract of Artocarpus heterophyllus, Murraya koenigii, and Punica granatum in polyethylene glycol ointment base. Three ointment formulations and six extracts with 5% and 10% extract concentration have been used. Excision wound rat model utilized for the wound healing potential. Results and Conclusion: All three plants, including A. heterophyllus Lam., M. koenigii Linn., and P. granatum Linn. extracted for the active constituent. The pharmacological evaluation on the excision wound healing model suggested that Group-I animals showed 52.09% of healing, whereas povidone-iodine treated animals showed 100.00% healing. On the other hand, the ointment formulation treated F-1 showed 96.47% of wound healing, F-2 showed 97.68% healing, and F-3 showed 99.11% healing. The overall healing results can be represented as following: Control <MKL5 <MKL10 <PGB5 <PGB10 <AHP5 <AHP10 <F-1 <F-2 <F-3 <Standard. F3 ointment formulation is better than the F2 and F1 formulation in wound healing potential as compared to others. Discussion: These studies have indicated that ointment formulations of A. heterophyllus, M. koenigii, P. granatum have been utilized for wound healing potential and it is safer for topical application. Excision wound healing model suggested that the three individual plant extract has shown the wound healing potential, although the prepared ointment formulations F3 have best and synergistic action than the individual. The ointment formulations containing plant extracts in 10% amount have better wound healing potential.
Characteristics of immobilized bacterial D-hydantoinase on alginate
Similar to Design, synthesis, characterization and biological evaluation of 3- (4-(7-chloro-2-(4-chlorophenyl)-4-oxo-quinazolin-3(4H)- yl)phenyl)-2-aryl 1,3-thiazolidin-4-ones as a new class of antimicrobial agents
Synthesis, Characterization and Biological Evaluation of Oxazolone Derivativesijceronline
A series of six 4-aryl Benzelidene-2-phenyl-5- oxazolone derivatives were synthesized by condensation of aromatic aldehydes with N-benzoyl glycine (Hippuric acid) in the presence of sodium acetate and acetic anhydride at room temperature in ethanol. Six of the compounds are new derivatives. The structures of the compounds were evaluated based on 1H-NMR , IR and FTIR methods and by elemental analysis. .All the derivative compounds prepared were tested for their antimicrobial activity by disk diffusion technique. Test organisms: Bacteria like Staphylococcus aureusMTCC 7443 and Salmonella typhimuriumMTCC 733 Fungi like C.albicans and A.flavus The results were compared with those of the standard 0.5% Ciprofloxacin. The derivatives with Salicylaldehyde and cinnamaldehyde were showed excellent activities against E. coli. and Staphylococcus aureusMTCC 7443 : than Salmonella typhimuriumMTCC 733 bacteria. It also showed reasonable activity withFungi like C.albicans than A.flavus
The Eco-friendly Marine Gastropod Turbo brunneus (L. 1758) and its Vital role...rahulmonikasharma
Molluscs form valuable fisheries in various parts of the coast of India providing shell fish as food and as source of lime, pearls and decorative shells, as constituents of medicinal preparations etc. In the present study, the eco-friendly Turbo brunneus and its vital role in future pharmaceutical industry through GC-MS analysis was carried out. Almost eighteen compounds are obtained through GC-MS which might be responsible for antimicrobial, pharmaceutical, insect repellent, anti-inflammatory, anticancer, antiasthmatic, diuretic and antiarthritic activities.
The Eco-friendly Marine Gastropod Turbo brunneus (L. 1758) and its Vital role...rahulmonikasharma
Molluscs form valuable fisheries in various parts of the coast of India providing shell fish as food and as source of lime, pearls and decorative shells, as constituents of medicinal preparations etc. In the present study, the eco-friendly Turbo brunneus and its vital role in future pharmaceutical industry through GC-MS analysis was carried out. Almost eighteen compounds are obtained through GC-MS which might be responsible for antimicrobial, pharmaceutical, insect repellent, anti-inflammatory, anticancer, antiasthmatic, diuretic and antiarthritic activities.
Anti Bacterial and Anti Oxidant Activities of Evolvulus Alsinoides LinnIOSRJPBS
: Plants are very important sources of potential useful raw materials as natural chemotherapeutic agents. Shankhpushpi is botanically termed as Evolvulus alsinoides; the extracts have exhibited antioxidant, anti-ulcer, and immunomodulatory activities. The present work is to investigate the invitro therapeutic potential activities of methanolic extract of whole plant of Evolvulus alsinoides on the antimicrobial activity against five clinical pathogenic bacterial strains viz., Staphylococcus aureus, Bacillus cereus, Escherichia coli, Klebshiella pneumonia and Salmonella typhii, using agar well diffusion assay and Anti oxidant activity using 1-1-Diphenyl- 2-picryl-hydrazyl (DPPH) radical. Extract inhibited IC50: 40.2. Total phenolic content: 28.4 mg/ml & Total flavonoid content: 20.2 μg /ml. Evolvulus alsinoides (MIC): 512.5mg/ml possess 30 to 40 % inhibition, the antibacterial activity of the herbal extracts was more pronounced on the gram- negative bacteria Klebshiella pneumonia than the gram-positive bacteria Staphylococcus aureus. The free radical scavenging activity of methanolic activity of whole plant of Evolvulus alsinoides increase in a concentration dependent manner, and posses statistically significance DPPH free radical scavenging & Anti microbial activities
Synthesis, Characterization and Biological Evaluation of Substitutedthiazolid...paperpublications3
Abstract: A new series of substituted thiazolidin-4-ones were synthesized and evaluated for anticancer activity by means of MTT assay method for improved anticancer activity .The structures of these synthesized compounds were established by means of IR,H NMR analysis.All the compounds were evaluated for their anticancer activity .Compounds TH10 & TH19 were found most active due to presence of electron withdrawing groups at appropriate position.
Novel Hybrid Molecules of Isoxazole Chalcone Derivatives: Synthesis and Study...Ratnakaram Venkata Nadh
medicine due to their significant role in the treatment of different health problems.
Methods: We have synthesized new series of isoxazole-chalcone conjugates (14a-m) by the
Claisen-Schmidt condensation of suitable substituted acetophenones with isoxazole aldehydes (12a-d).
In vitro cytotoxic activity of the synthesized compounds was studied against four different selected
human cancer cell lines by using sulforhodamine B (SRB) method.
Results: The adopted scheme resulted in good yields of new series of isoxazole-chalcone
conjugates (14a-m). Potent cytotoxic activity was observed for compounds -14a, 14b, 14e, 14i, 14j
and 14k against prostate DU-145 cancer cell line.
Conclusion: The observed potent cytotoxic activities were due to the presence of 3,4,5-
trimethoxyphenyl group.
Design, Synthesis, and Characterization of New 1,3,5-Trisubstituted-2-pyrazol...BRNSS Publication Hub
Objective: The objective of the paper was to design, synthesis, and characterization of new 1,3,5-trisubstituted-2-pyrazolines derivative and to evaluate for analgesic potential. Materials and Methods: The 1,3,5-tri-substituted-2-pyrazolines derivatives have been synthesized by the reaction of chalcone derivatives with 4-hydrazinylbenzene sulfonamide hydrochloride and phenyl hydrazine hydrochloride. Total 16 compounds have been synthesized and characterized by the IR, 1HNMR, and mass spectral analysis. Proposed compounds have been evaluated for analgesic activity. The synthesized compounds also evaluated for the analgesic activity by the following two methods, that is, hot plate test method and acetic acid induced writhing in mice. Pentazocine and acetyl acetic acid were used as standard drug for compare the efficacy. Results and Discussion: The analgesic activity of the 16 synthesized compound series A1-A8, and B1-B8 has been evaluated using hot plate test method and acetic acid induced writhing in mice. The results of the evaluation have been viewed by taking pentazocine and acetyl acetic acid as the standard drug. In hot plate test, series A1-A8, shown delay the paw withdrawal latency time for compound A2 (10.30 s), A4 (9.45 s), A7 (11.65 s), and A8 (11.26 s) after 90 min. In series, B1-B8 shown delay the paw withdrawal latency time for compound B2 (9.10 s) and B7 (10.42 s) after 90 min, inhibit the pain sensation, and inhibit pain produced by thermal means. Synthesized compounds of series A1-A8, compounds A2, A5, A6, A7, and A8 were shown 83.00, 76.01, 80.34, 86.99, and 88.15 were shown percent inhibition, significantly (p<0.05 and p<0.001, respectively) and reduced the number of wriths induced by 0.6% acetic acid at the dose of 10 mg/kg. Acetylsalicylic acid (10 mg/kg) appears to be better effective in reducing the number of wriths, it significantly (P < 0.001) reduced the number of wriths by 99.0%. The compounds B1, B3, and B4 have shown least active activity. These all finding suggest that these synthesized compounds have the potential as analgesic agent. Conclusion: The 1,3,5-pyrazoline derivatives has been successfully synthesized and evaluated for analgesic activity of mice model and results data indicate that compounds A2, A5, A6, A7, and A8 were shown 83.00, 76.01, 80.34, 86.99, and 88.15%, and compounds B2, B7, and B8 were shown 72.25, 74.27, and 74.56% inhibitions. The presence of SO2NH2 is essential for analgesic activity.
Synthesis, Characterization and Biological Evaluation of Substituted Thiazoli...paperpublications3
Abstract: A new series of substituted thiazolidin-4-ones were synthesized and evaluated for antimicrobial activity by means of zone of inhibition by cup plate method. The structures of these compounds were established by means by IR, H NMR analysis. All the compounds were evaluated for their antibacterial activity against gram positive and gram negative species and antifungal activity .Compounds TH09 & TH17 were found most active due to presence of electron withdrawing groups at appropriate position.
Synthesis and Anti-Inflammatory activity of Sulpha/substituted 1,2-Diazolesinventionjournals
A Novel compound namely N1 (3 Nicotinoyl) 3,5 dimethyl-4-(N-4-sulfamoyl-azo)-1,2-diazoles has been synthesized by two step processes. Synthesis of N1 -4-sulfamoylphenylhydrazono-3,5-dimethyl propane-1,3-dione and sulfonamide, which interacting with 3-Nicotinoyl hydrazine to form final compound. The newly synthesized compound N1 -(3-Nicotinoyl)-3,5-dimethyl 4-(N1 -4-sulfamoyl phenyl azo) 1,2-diazoles was screened for antiinflammatory activity
Synthesis and Anti-Inflammatory activity of Sulpha/substituted 1,2-Diazolesinventionjournals
A Novel compound namely N1 (3 Nicotinoyl) 3,5 dimethyl-4-(N-4-sulfamoyl-azo)-1,2-diazoles has been synthesized by two step processes. Synthesis of N1 -4-sulfamoylphenylhydrazono-3,5-dimethyl propane-1,3-dione and sulfonamide, which interacting with 3-Nicotinoyl hydrazine to form final compound. The newly synthesized compound N1 -(3-Nicotinoyl)-3,5-dimethyl 4-(N1 -4-sulfamoyl phenyl azo) 1,2-diazoles was screened for antiinflammatory activity
New Derivatives of (E)-3-(5-((substitutedphenylamino)methyl)-1,3,4-thiadiazol...BRNSS Publication Hub
Objective: The objective of the paper was to evaluate the antifungal and antibacterial potential of new derivatives of ((E)-3-(5-((substitutedphenylamino)methyl)-1,3,4-thiadiazol-2-yl)-2-styryl quinazolin-4(3H)-one. Materials and Methods: Various syntheses of (E)-3-(5-(substitutedaminomethyl)-1,3,4-thiadiazol-2-yl)-2-styrylquinazolin-4(3H)-one derivatives have been synthesized by reacting 2-substituted benzoxazin-4-one with (E)-2-(4-Substituedstyryl)-4H-benzo[d] [1,3]oxazin-4-one. All synthesized compounds have been characterized by the infrared, 1HNMR, and mass spectral analysis. Proposed compounds have been evaluated for antifungal and antibacterial activity. The antimicrobial activity of synthesized compounds (QNM-1 to QNM-15) has been carried through the serial dilution method. For bacterial screening, bacterial species were taken includes Staphylococcus aureus (MTCC-96), Bacillus subtilis (MTCC-441), Pseudomonas aeruginosa (MTCC-424), and Escherichia coli (MTCC-40). Norfloxacin (1-Ethyl-6-fluoro-1,4,dihydro-4-oxo-7-(1-piperazinyl)-3-quinoline carboxylic acid) was used as the standard drug for antibacterial study. For antifungal screening, the following fungal species were used includes Aspergillus niger (MTCC-281), Candida albicans (MTCC-227), and Fusarium oxysporum (MTCC-284). Clotrimazole was selected as a standard drug for antifungal study. Results and Discussion: QNM-1, QNM-2, QNM-3, QNM-5, QNM-7, QNM-9, QNM-12, QNM-14, and QNM-15 were the most active compounds [Table 1] in the synthesized series which were active against both Gram-positive and Gram-negative organisms by the antibacterial screening. In the case of antibacterial activity, the presence of electronegative group (Cl, Br, F, and NO2) at both R may enhance the activity when they are p-substituted, but the compounds QNM-6 (R1=-C6H5Br (o); Ar=-C6H5), QNM-10 (R1 = -C6H5F (o); Ar= -C6H5F), QNM-11 (R1 =-C6H5NO2 (p); Ar=-C6H5F), and QNM-4 (R1 =-C6H5F (m); Ar=-C6H5) with given substitution may result in diminishing the activity. In case of antifungal activity, compounds QNM-1, QNM-5, QNM-7, QNM-9, QNM-11, QNM-12, QNM-14, and QNM-15 were the most active compounds in the synthesized series which were active against both Gram-positive and Gram-negative organisms. In that series, compounds QNM-14, QNM-11, QNM-5, and QNM-7 have shown the highest activity. Compounds QNM-3, QNM-6, QNM-10, and QNM-13 have the least active. This result has also concluded that o-substituted compounds, i.e., -C6H5Cl(o), -C6H5Cl (m), -C6H5Br(o), -C6H5F (o), -C6H5F (p) at R1 position my resulted in diminishing or lower the activity.
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.
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Does Goods and Services Tax (GST) Leads to Indian Economic Development?iosrjce
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Customer’s Acceptance of Internet Banking in Dubaiiosrjce
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THE IMPORTANCE OF MARTIAN ATMOSPHERE SAMPLE RETURN.Sérgio Sacani
The return of a sample of near-surface atmosphere from Mars would facilitate answers to several first-order science questions surrounding the formation and evolution of the planet. One of the important aspects of terrestrial planet formation in general is the role that primary atmospheres played in influencing the chemistry and structure of the planets and their antecedents. Studies of the martian atmosphere can be used to investigate the role of a primary atmosphere in its history. Atmosphere samples would also inform our understanding of the near-surface chemistry of the planet, and ultimately the prospects for life. High-precision isotopic analyses of constituent gases are needed to address these questions, requiring that the analyses are made on returned samples rather than in situ.
Introduction:
RNA interference (RNAi) or Post-Transcriptional Gene Silencing (PTGS) is an important biological process for modulating eukaryotic gene expression.
It is highly conserved process of posttranscriptional gene silencing by which double stranded RNA (dsRNA) causes sequence-specific degradation of mRNA sequences.
dsRNA-induced gene silencing (RNAi) is reported in a wide range of eukaryotes ranging from worms, insects, mammals and plants.
This process mediates resistance to both endogenous parasitic and exogenous pathogenic nucleic acids, and regulates the expression of protein-coding genes.
What are small ncRNAs?
micro RNA (miRNA)
short interfering RNA (siRNA)
Properties of small non-coding RNA:
Involved in silencing mRNA transcripts.
Called “small” because they are usually only about 21-24 nucleotides long.
Synthesized by first cutting up longer precursor sequences (like the 61nt one that Lee discovered).
Silence an mRNA by base pairing with some sequence on the mRNA.
Discovery of siRNA?
The first small RNA:
In 1993 Rosalind Lee (Victor Ambros lab) was studying a non- coding gene in C. elegans, lin-4, that was involved in silencing of another gene, lin-14, at the appropriate time in the
development of the worm C. elegans.
Two small transcripts of lin-4 (22nt and 61nt) were found to be complementary to a sequence in the 3' UTR of lin-14.
Because lin-4 encoded no protein, she deduced that it must be these transcripts that are causing the silencing by RNA-RNA interactions.
Types of RNAi ( non coding RNA)
MiRNA
Length (23-25 nt)
Trans acting
Binds with target MRNA in mismatch
Translation inhibition
Si RNA
Length 21 nt.
Cis acting
Bind with target Mrna in perfect complementary sequence
Piwi-RNA
Length ; 25 to 36 nt.
Expressed in Germ Cells
Regulates trnasposomes activity
MECHANISM OF RNAI:
First the double-stranded RNA teams up with a protein complex named Dicer, which cuts the long RNA into short pieces.
Then another protein complex called RISC (RNA-induced silencing complex) discards one of the two RNA strands.
The RISC-docked, single-stranded RNA then pairs with the homologous mRNA and destroys it.
THE RISC COMPLEX:
RISC is large(>500kD) RNA multi- protein Binding complex which triggers MRNA degradation in response to MRNA
Unwinding of double stranded Si RNA by ATP independent Helicase
Active component of RISC is Ago proteins( ENDONUCLEASE) which cleave target MRNA.
DICER: endonuclease (RNase Family III)
Argonaute: Central Component of the RNA-Induced Silencing Complex (RISC)
One strand of the dsRNA produced by Dicer is retained in the RISC complex in association with Argonaute
ARGONAUTE PROTEIN :
1.PAZ(PIWI/Argonaute/ Zwille)- Recognition of target MRNA
2.PIWI (p-element induced wimpy Testis)- breaks Phosphodiester bond of mRNA.)RNAse H activity.
MiRNA:
The Double-stranded RNAs are naturally produced in eukaryotic cells during development, and they have a key role in regulating gene expression .
Richard's entangled aventures in wonderlandRichard Gill
Since the loophole-free Bell experiments of 2020 and the Nobel prizes in physics of 2022, critics of Bell's work have retreated to the fortress of super-determinism. Now, super-determinism is a derogatory word - it just means "determinism". Palmer, Hance and Hossenfelder argue that quantum mechanics and determinism are not incompatible, using a sophisticated mathematical construction based on a subtle thinning of allowed states and measurements in quantum mechanics, such that what is left appears to make Bell's argument fail, without altering the empirical predictions of quantum mechanics. I think however that it is a smoke screen, and the slogan "lost in math" comes to my mind. I will discuss some other recent disproofs of Bell's theorem using the language of causality based on causal graphs. Causal thinking is also central to law and justice. I will mention surprising connections to my work on serial killer nurse cases, in particular the Dutch case of Lucia de Berk and the current UK case of Lucy Letby.
Multi-source connectivity as the driver of solar wind variability in the heli...Sérgio Sacani
The ambient solar wind that flls the heliosphere originates from multiple
sources in the solar corona and is highly structured. It is often described
as high-speed, relatively homogeneous, plasma streams from coronal
holes and slow-speed, highly variable, streams whose source regions are
under debate. A key goal of ESA/NASA’s Solar Orbiter mission is to identify
solar wind sources and understand what drives the complexity seen in the
heliosphere. By combining magnetic feld modelling and spectroscopic
techniques with high-resolution observations and measurements, we show
that the solar wind variability detected in situ by Solar Orbiter in March
2022 is driven by spatio-temporal changes in the magnetic connectivity to
multiple sources in the solar atmosphere. The magnetic feld footpoints
connected to the spacecraft moved from the boundaries of a coronal hole
to one active region (12961) and then across to another region (12957). This
is refected in the in situ measurements, which show the transition from fast
to highly Alfvénic then to slow solar wind that is disrupted by the arrival of
a coronal mass ejection. Our results describe solar wind variability at 0.5 au
but are applicable to near-Earth observatories.
Professional air quality monitoring systems provide immediate, on-site data for analysis, compliance, and decision-making.
Monitor common gases, weather parameters, particulates.
This presentation explores a brief idea about the structural and functional attributes of nucleotides, the structure and function of genetic materials along with the impact of UV rays and pH upon them.
PRESENTATION ABOUT PRINCIPLE OF COSMATIC EVALUATION
Design, synthesis, characterization and biological evaluation of 3- (4-(7-chloro-2-(4-chlorophenyl)-4-oxo-quinazolin-3(4H)- yl)phenyl)-2-aryl 1,3-thiazolidin-4-ones as a new class of antimicrobial agents
1. IOSR Journal of Pharmacy and Biological Sciences (IOSR-JPBS)
e-ISSN: 2278-3008, p-ISSN:2319-7676. Volume 10, Issue 1 Ver. IV (Jan -Feb. 2015), PP 30-36
www.iosrjournals.org
DOI: 10.9790/3008-10143036 www.iosrjournals.org 30 | Page
Design, synthesis, characterization and biological evaluation of 3-
(4-(7-chloro-2-(4-chlorophenyl)-4-oxo-quinazolin-3(4H)-
yl)phenyl)-2-aryl 1,3-thiazolidin-4-ones as a new class of
antimicrobial agents
P. Bharath Rathna Kumar1
, M. Srinivasa Murthy2
and K.N Jayaveera3
1Department of Pharmaceutical Chemistry, Oil Technological Research Institute- JNTUA, Ananthapuramu,
A.P, India.
2Department of Pharmaceutical Chemistry, Vignan Institute of Pharmaceutical Sciences, Deshmukhi,
Nalgonda, A.P, India.
3Director, Research and Development, Adept Pharma and Bioscience Excellence Pvt., Ltd, Hyderabad, A.P,
India
Abstract: 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.
Key Words: Thiazolidinone, quinazolinone, benzoxazinone, synthesis, characterization.
I. Introduction
The usage of most of the antimicrobial agents is limited, not only by the rapidly developing drug
resistance, but also by the unsatisfactory status of present treatments of bacterial and fungal infections and drug
side effects. This has spewed the scientists to develop the new antibacterial agents having broad antimicrobial
spectrum. In the present research work we reported the synthesis of some new thiazolidinone derivatives by
using various substituted aromatic aldehydes and screened for their anti-microbial activity. Thiazolidinones are
derivatives of thiazolidine and are significant group of heterocyclic compounds. There are three types of
thiazolidinones based on 2nd
, 4th
and 5th
position of carbonyl group. The most significant one is thiozolidinone
with carbonyl group at 4th
position, which is also known as 4-thiazolidinone or 4-oxo-thiazolidine. Thiazolidin-
4-ones and their derivatives have attracted much attention due to diverse biological activities such as
antidiabetic1
, antihistaminic2,3
, Ca2+
-channel blocker4
, anti-platelet activating factor5,6
, antidiarrheal7
, platelet
activating factor (PAF) antagonist8
, cardioprotective9
, anti-ischemic10
, cyclooxygenase (COX) inhibitory11
, anti-
cancer12
, nematicidal13
and convulsant14
activities. Quinazolinone is a important heterocyclic ring with broad
spectrum of biological activities like anticonvulsant15
, analgesic16
, antitumor17
, anti-inflammatory18
,
antimicrobial19
, antitubercular20
, antioxidant21
and antiviral22
activities. In view of antimicrobial activities of
some thiazolidinone derivatives and quinazolinone derivatives it was of curiosity to couple these two moieties
with the hope that the resulting compounds might exhibit superior activity. After a comprehensive literature
survey our focus was to synthesise thiazolidinone derivatives as less toxic, more active antimicrobial agents
(Fig. 1). The synthetic strategies adopted for the synthesis of the intermediate and target compounds are
depicted in the Scheme I.
2. Design, synthesis, characterization and biological evaluation of 3-(4-(7-chloro-2-(4-chlorophenyl)....
DOI: 10.9790/3008-10143036 www.iosrjournals.org 31 | Page
S
N
O
N
N
O
Cl
Cl
OH
S
N
O
N
N
O
Cl
Cl
O CH3
S
N
O
N
N
O
Cl
Cl
O
O
CH3
CH3
O
CH3
TQVI(4) TQVI(5) TQVI(6)
Figure 1. Structures of the most active compounds.
COOH
NH2Cl
O
N
O
Cl
Cl
+
TQ-I TQ-III
O
Cl
Cl
2-amino-4-chlorobenz
oic acid 7-chloro-2-(4-chlorophenyl)
-4H-3,1-benzoxazin-4-one
p-chloro benzoyl
chloride
TQ-II
N
N
O
NH2
Cl
Cl
TQIV
3-(4-aminophenyl)-7-chloro-2-(4-c
hlorophenyl)quinazolin-4(3H)-one
N
N
O
N
Cl
Cl
N
N
O
N
S
O
Cl
Cl
TQVI(1-10)
3-(4-(7-chloro-2-(4-chlorophenyl)4-oxo
-quinazolin-3(4H)-yl)phenyl)-2-arylthi
azolidin-4-one
7-chloro-2-(4-chlorophenyl)-3-(
4-{[(E)-arylmethylidene]amino}p
henyl)quinazolin-4(3H)-one
TQV(1-10)
a
b
c
d
R = H-,
4-Cl-,
3-NO2-,
4-OH-,
4-OCH3-,
3,4,5-(OCH3)3-,
3,4-(OCH3)2-,
4-F-
4-CH2CH3
4-CH(CH3)2
R
R
Scheme I. Reagents and condition: (a) Pyridine, NaHCO3, Stirr for 30min; (b) Pyridine,HCl, p-
phenylenediamine, Reflux for 6h; (c) aryl aldehyde, Ethanol, Glacial acetic acid, Reflux for 8h; (d) DMF,
ZnCl2, HSCH2COOH, Reflux for 8h;
3. Design, synthesis, characterization and biological evaluation of 3-(4-(7-chloro-2-(4-chlorophenyl)....
DOI: 10.9790/3008-10143036 www.iosrjournals.org 32 | Page
II. Materials And Methods
In the present study the title compounds were examined for in vitro antimicrobial potency against four
bacterial pathogens and two fungal pathogens. Bacterial and fungal strains (Microbial Type Culture Collection,
MTCC) were purchased from IMTECH, Chandigarh, India. Ampicillin and Amphotericin B were procured from
Sigma Aldrich, Bangalore, India. Samples were routinely purified by crystallization from ethanol. Melting
points were taken in open capillaries and are uncorrected. The purity of compounds was checked by TLC on
silica gel „G‟ coated glass plates. IR spectra were recorded in BRUKER ATR-IR spectrophotometer. 1
H-NMR
spectra (DMSO) were recorded on NEW AVANCE− (300 MHZ) NMR spectrometer using TMS as internal
standard. Mass spectra of the synthesized compounds have been recorded on a VG Autospec MS using
ESI+
software with capillary voltage 3.98 kV and ESI mode positive ion trap detector. Chloroform and
ethylacetate in the ratio 7:3 was used as mobile phase for elution and the spots were detected in iodine chamber.
III. Experimental
General procedure for synthesis of 7-chloro-2-(4-chlorophenyl)-4H-3, 1-benzoxazin-4-one TQ-III23,24
:
2-Amino-4-chlorobenzoic acid (0.1 mol) was dissolved in 30ml of dry pyridine by stirring slowly at room
temperature. The solution was cooled to 0°C and a solution of a p-chloro benzoyl chloride (0.2 mol) in 30ml of
dry pyridine was added slowly with constant stirring. After this addition the reaction mixture was further stirred
for half an hour at room temperature and set aside for 1h. The pasty mass obtained was diluted with 50 ml of
water and treated with aqueous sodium bicarbonate solution. When the effervescence ceased, the precipitate
obtained was filtered and washed with water. The crude 7-chloro-2-(4-chlorophenyl)-4H-3, 1-benzoxazin-4-one
obtained was dried and recrystallized from diluted ethanol (m.p:155-157), yield (92%).
General procedure for synthesis of 3-(4-aminophenyl)-7-chloro-2-(4-chlorophenyl)-quinazolin-
4(3H)-one TQ-IV25
: 7-chloro-2-(4-chlorophenyl)-4H-3,1-benzoxazin-4-one (0.01mol) and p-phenylenediamine
(1.08 g, 0.01 mol) was dissolved in 50 mL of anhydrous pyridine and refluxed for 6 h. The resulting solution
was cooled in ice bath and treated with 100 mL of dilute hydrochloric acid. The obtained crude precipitate of 3-
(4-aminophenyl)-7-chloro-2-(4-chlorophenyl)quinazolin-4(3H)-one was filtered, washed with water and
recrystallized from ethanol (m.p:165-167), yield (85-90%).
General procedure for synthesis of 7-chloro-2-(4-chlorophenyl)-3-(4-{[(E)-arylmethylidene]
amino} phenyl) quinazolin-4(3H)-one TQ-V (1-10)26
: 3-(4-aminophenyl)-7-chloro-2-(4-chlorophenyl)
quinazolin-4(3H)-one TQ-IV (0.01 mol) and aromatic aldehydes (0.01 mol) were dissolved in absolute ethanol
(50 ml), by the addition of a few drops of glacial acetic acid. The reaction mixture was refluxed for 8h. The
reaction mixture was allowed to cool and poured into ice cold water. The separated solid was filtered, washed
and recrystallized from ethanol.
General procedure for the synthesis of 3-(4-(7-chloro-2-(4-chlorophenyl)4-oxo-quinazolin-3(4H)-
yl)phenyl)-2-arylthiazolidin-4-one TQ-VI(1-10)27
: 7-chloro-2-(4-chlorophenyl)-3-(4-{[(E)-arylmethylidene]
amino} phenyl) quinazolin-4(3H)-one TQ-V (A-G) (0.01 mol) were dissolved in dry DMF (50 ml), containing a
pinch of anhydrous ZnCl2 and thioglycolic acid (0.02 mol) and refluxed for about 8h. Excess of solvent was
distilled off and the residual reaction mixture cooled and poured into ice cold water. The separated solid was
filtered, washed and recrystallized from ethanol.
IV. Results And Discussions
Spectral data of synthesized compounds TQVI (1-10):
3-(4-(7-chloro-2-(4-chlorophenyl)4-oxo-quinazolin-3(4H)-yl)phenyl)-2-phenyl thiazolidin-4-one
TQVI(1): ATR-IR (vmax cm−1
): 1730 -C=O stretching; 1662 -C=O stretching; 1517 -C=N stretching; 3085 -C-H
aromatic stretching; 812 -C-Cl stretching; 1370 -NCS stretching; 1
HNMR δppm 300 MHz, DMSO-d6: δ5.9 (s, -
CH-Ar, 1H), δ3.7 (s, -CH2-S- 2H), δ6.7-8.8 (m, Ar-H and quinazoline-H, 16H). MS: m/z 544(M+
).
3-(4-(7-chloro-2-(4-chlorophenyl)-4-oxo-quinazolin-3-(4H)-yl)phenyl)-2-(4-chlorophenyl)
thiazolidin-4-one TQVI(2): ATR-IR (vmax cm−1
): 1703 -C=O stretching; 1665 -C=O stretching; 1519 -C=N
stretching; 3093 -C-H aromatic stretching; 816 C-Cl stretching; 1363 -NCS stretching; 1
HNMR δppm 300
MHz, DMSO-d6: δ6.0 (s, -CH-Ar, 1H), δ3.5 (s, -CH2-S, 2H), δ6.3-9.0 (m, Ar-H, 15H and quinazoline-H) MS:
m/
3-(4-(7-chloro-2-(4-chlorophenyl)-4-oxo-quinazolin-3-(4H)-yl)phenyl)-2-(3-nitrophenyl)
thiazolidin-4-one (TQVI(3): ATR-IR (vmax cm−1
): 1730 -C=O stretching; 1661 -C=O stretching; 1510 -C=N
stretching; 3049 -C-H Aromatic stretching; 812 -C-Cl stretching; 1377 –N-C-S stretching;. 1
HNMR δppm 300
MHz, DMSO-d6: δ6.2 (s, 1H, -CH-Ar), 3.4(s, 2H, -CH2-S-), δ7.2-8.9 (m, Ar-H and quinazoline-H, 15H) MS:
m/z 589 (M+
).
3-(4-(7-chloro-2-(4-chlorophenyl)4-oxo-quinazolin-3-(4H)-yl)phenyl)-2-(4-hydroxyphenyl)
thiazolidin-4-one TQVI(4): ATR-IR (vmax cm−1
): 1740 -C=O stretching; 1654 -C=O stretching; 1503 -C=N
stretching; 3074 -C-H aromatic stretching; 827 -C-Cl stretching; 3389 -OH stretching; 1242 –N-C-S) stretching;
4. Design, synthesis, characterization and biological evaluation of 3-(4-(7-chloro-2-(4-chlorophenyl)....
DOI: 10.9790/3008-10143036 www.iosrjournals.org 33 | Page
1
HNMR δppm 300 MHz, DMSO-d6: δ6.1 (s, 1H, -CH-Ar), δ3.7 (s, 2H, -CH2-S-), δ6.4-8.3 (m, Ar-H and
quinazoline –H, 15H) MS: m/z 526 (M+
).
3-(4-(7-chloro-2- (4-chlorophenyl) 4-oxo-quinazolin-3-(4H)-yl) phenyl)-2-(4-methoxyphenyl)
thiazolidin-4-one TQVI(5): ATR-IR (vmax cm−1
): 1736 -C=O stretching; 1656 -C=O stretching; 1504 -C=N
stretching; 1504 -C=C stretching; 3085 -C-H aromatic stretching; 2920, 2851-C-H aliphatic stretching; 826 -C-
Cl stretching; 1243 -C-O-C stretching; 1362 -N-C-S stretching; 1
HNMR δppm 300 MHz, DMSO-d6: δ6.4 (s, -
CH-Ar, 1H), δ3.3 (s, -CH2-S, 2H), δ6.7-8.8 (m, Ar-H and quinazoline-H, 15H), δ2.7 (s, -OCH3, 3H) MS: m/z
574 (M+
).
3-(4-(7-chloro-2-(4-chlorophenyl)4-oxo-quinazolin-3-(4H)-yl)phenyl)-2-(3,4,5-trimethoxyphenyl)
thiazolidin-4-one TQVI(6): ATR-IR (vmax cm−1
): 3089 -C-H aromatic stretching; 2917,2848 -C-H aliphatic
stretching; 1741 -C=O stretching; 1655 -C=O stretching; 1504 -C=N stretching; 826 -C-Cl stretching; 1244 -C-
O-C stretching; 1362 -N-C-S stretching; 1
HNMR δppm 300 MHz, DMSO-d6: δ6.0 (s, -CH-Ar, 1H), δ3.9 (s, -
CH2-S, 2H), δ6.5-8.4 (m, Ar-H and quinazoline-H, 13H) δ2.5 (s, 9H, -(OCH3)3). MS: m/z 635 (M+
).
3-(4-(7-chloro-2-(4-chlorophenyl)4-oxo-quinazolin-3-(4H)-yl)phenyl)-2-(3,4-dimethoxyphenyl)
thiazolidin-4-one TQVI(7): ATR-IR (vmax cm−1
): 3067 -C-H aromatic stretching; 2932,2873 -C-H aliphatic
stretching; 1729 -C=O stretching; 1636 -C=O stretching; 1505 -C=N stretching; 831 -C-Cl stretching; 1244 -C-
O-C stretching; 1373 -N-C-S stretching; 1
HNMR δppm 300 MHz, DMSO-d6: δ5.9 (s, -CH-Ar, 1H), δ4.0 (s,
CH2-S, 2H), δ6.5-8.0 (m, Ar-H and quinazoline-H, 15H) δ2.5 (s, 6H, -(OCH3)2). MS: m/z 605 (M+
).
3-(4-(7-chloro-2-(4-chlorophenyl)4-oxo-quinazolin-3-(4H)-yl)phenyl)-2-(4-fluorophenyl)
thiazolidin-4-one TQVI(8): ATR-IR (vmax cm−1
): 1736 -C=O stretching, 1656 -C=O stretching, 1504 -C=N
stretching, 3075 -C-H aromatic stretching, 826 -C-Cl stretching, 1362 –NCS stretching. 1
HNMR δppm 300
MHz, DMSO-d6: δ5.9 (s, -CH-Ar, 1H), δ3.7 (s, CH2-S, 2H), δ7.0-9.0 (m, Ar-H and quinazoline-H, 15H) MS:
m/z 562 (M+
).
3-(4-(7-chloro-2-(4-chlorophenyl)4-oxo-quinazolin-3-(4H)-yl)phenyl)-2-(4-ethylphenyl)
thiazolidin-4-one TQVI(9): ATR-IR (vmax cm−1
): 3055 -C-H aromatic stretching; 2964,2837 -C-H aliphatic
stretching; 1703 -C=O stretching; 1693 -C=O stretching; 823 -C-Cl stretching; 1244 -C-O-C stretching; 1322 -
N-C-S stretching; 1
HNMR δppm 300 MHz, DMSO-d6: δ5.8 (s, -CH-Ar, 1H), δ3.0 (s, -CH2-S, 2H), δ6.2-8.0 (m,
Ar-H and quinazoline-H, 15H), δ2.1-2.4 (q, -CH2, 2H), δ1.7 (t, -CH3, 3H). MS: m/z 573 (M+
).
3-(4-(7-chloro-2-(4-chlorophenyl)4-oxo-quinazolin-3-(4H)-yl)phenyl)-2-(4-isopropylphenyl)
thiazolidin-4-one TQVI(10): ATR-IR (vmax cm−1
): 3097 -C-H aromatic stretching; 2916,2794 -C-H aliphatic
stretching; 1745 -C=O stretching; 1662 -C=O stretching; 825 -C-Cl stretching; 1260 -C-O-C stretching; 1320 –
N-C-S stretching;. 1
HNMR δppm 300 MHz, DMSO-d6: δ5.8 (s, -CH-Ar, 1H), δ3.9 (s, -CH2-S, 2H), δ7.0-8.4
(m, Ar-H and quinazoline-H, 15H), δ2.0 (s, -N(CH3)2, 6H). MS: m/z 588 (M+
).
Antimicrobial activity - cup plate method28
The antimicrobial screening of synthesized compounds was performed using the cup plate method.
Nutrient broth media and Sabouraud‟s dextrose was prepared sterilized by autoclaving and was transferred into
sterile Petri plates. After solidification of media, cups of diameter 8mm were made with a sterile cork borer. 200
μl of the standardized29
bacterial inoculums and fungus inoculums containing about 3.0 × 105
cfu/ml were
spread on medium using bent glass rod. The synthesized compounds were dissolved in DMF to get a final
concentration 100µg/0.1ml and tested for activity. Ampicillin and Amphotericin B were used as a standard for
the antibacterial and antifungal activity, respectively. All the bacterial Petri plates were kept in incubator at
37±1°C and the fungal Petri plate was in an incubator at 24±1°C. Then the zones of inhibition of bacterial and
fungal growth were measured by using a transparent ruler.
Antibacterial and antifungal activity of all the synthesized compounds was screened against two gram-
positive bacterial strains (S.aureus & B.subtilis) and two gram-negative (E.coli & P.aeruginosa) bacterial strains,
two fungal strains (A.niger & C.albicans) at a concentration of 100 μg/0.1ml using cup plate method. The MIC
level of compounds TQ-VI (1-10) against these organisms is given in Table 2. The screening results of
antibacterial activities showed that the compound with TQ-VI4, TQ-VI5, TQ-VI6 with 4-OH, 4-OCH3 and
3,4,5-(OCH3)3 substituent‟s respectively showed potent activity against A.niger. Compound TQ-VI4 bearing 4-
OH substituent showed good activity against C.albicans. Compounds TQ-VI2, TQ-VI5 with 4-Cl and 4-OCH3
substituent‟s showed good activity against E.Coli and P.aeruginosa. Other compounds showed mild to moderate
antibacterial and antifungal activity. Structure of compounds TQ-V (1-10) and TQ-VI (1-10) was established on
the basis of spectral data. The IR spectra of TQ-VI (1-10) showed absence of absorption in the region 1500-
1525 cm-1
which confirms the absence of –CH=N- and presence of absorption band in the range 1730-1740 cm-1
due to C=O of thiazolidinone.1
H NMR spectra of compounds TQ-V (1-10) showed a singlet of –N=CH- at 6.00,
and presence of a a singlet of –CH2-S- at 3.65 in compounds TQ-VI (1-10) confirms the formation of TQ-VI
(1-10).
5. Design, synthesis, characterization and biological evaluation of 3-(4-(7-chloro-2-(4-chlorophenyl)....
DOI: 10.9790/3008-10143036 www.iosrjournals.org 34 | Page
Acknowledgement
The authors thank Prof.Dr.N.Devanna, Director, Oil Technological Research Institute, JNTUA,
Ananthapuramu for the encouragement and facilities provided to carry out this research work. We also thank the
IICT, Hyderabad for providing spectral data.
V. Conclusion
In the present paper, we report the synthesis, spectral studies, evaluation of antimicrobial activity of 3-
(4-(7-chloro-2-(4-chlorophenyl)-4-oxo-quinazolin-3-(4H)-yl) phenyl)-2-arylthiazolidin-4-one TQ-VI(1-
10).Thus these compounds constitute an interesting template for the evaluation of antimicrobial activity. In
conclusion, we reported herein a simple and convenient route for the synthesis of some new heterocyclic
compounds based on thiazolidinone for antimicrobial evaluation.
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Table-1: Physicochemical Characterization Of Newly Synthesized Compounds TQ-V (1-10) And TQ-VI (1-10)
Table 2: In Vitro Antibacterial And Antifungal Activity (Quantitative Study) Of The Synthesized Compounds
TQ-VI(1-10)
Compound R
Antibacterial Activity (MICa
in µg/ml)
S.aureusb
B.subtilisb
E.colib
P.aeruginosab
A.nigerc
C.albicansc
TQVI(1) H- 500 1000 500 500 500 500
TQVI(2) 4-Cl- 500 500 250 125 500 125
TQVI(3) 3-NO2- 500 1000 1000 1000 125 500
TQVI(4) 4-OH- 500 1000 500 500 31.25 62.5
TQVI(5) 4-OCH3- 250 125 125 62.5 31.25 125
TQVI(6) 3,4,5-(OCH3)3- 125 125 125 62.5 62.5 125
TQVI(7) 3,4-(OCH3)2- 125 125 500 125 62.5 125
TQVI(8) 4-F- 250 500 125 125 125 62.5
TQVI(9) 4-CH2CH3 500 1000 500 1000 62.5 250
TQVI(10) 4-CH(CH3)2 500 500 1000 1000 62.5 62.5
DMFd
- - - - - - -
Ampicillin - 1.95 1.95 7.81 15.62 - -
Amphotericin B - - - - - 3.90 7.81
a
The MIC value is defined as lowest concentration of the antifungal agent exhibiting no fungal growth. b
Bacteria tested: Staphylococcus aureus (MTCC 3160) and Bacillus subtilis (MTCC 441). Escherichia coli
(MTCC 443) and Pseudomonas aeruginosa (MTCC 424).
c
Fungi tested : Aspergillus niger (MTCC 282) and Candida albicans (MTCC 227)
d
DMF: Dimethyl formamide.
TABLE 3: In Vitro Antibacterial And Antifungal Activity (Qualitative Study) Of The Synthesized Compounds
TQ-VI(1-10)
Compound R
Antibacterial Activity (Zone of inhibition in mm)a
S.aureusb
B.subtilisb
E.colib
P.aeruginosab
A.nigerc
C.albicansc
TQVI(1) H- 09 8 16 12 06 08
TQVI(2) 4-Cl- 16 17 16 20 07 12
TQVI(3) 3-NO2- 10 06 08 10 11 06
TQVI(4) 4-OH- 13 8 18 11 16 15
TQVI(5) 4-OCH3- 18 21 21 24 17 11
Compound Molecular formula Molecular
Weight
Melting point
( o
C )
% yield Rf value
TQV(1) C27H17Cl2N3O 470.3 144-145 75 0.69
TQV(2) C27H16Cl3N3O 504.7 216-217 78 0.71
TQV(3) C27H16Cl2N4O3 515.3 168-169 70 0.73
TQV(4) C27H17Cl2N3O2 486.3 188-189 67 0.63
TQV(5) C28H19Cl2N3O2 500.3 286-287 73 0.68
TQV(6) C30H23Cl2N3O4 560.4 256-257 75 0.65
TQV(7) C29H21Cl2N3O3 530.4 252-253 78 0.78
TQV(8) C27H16Cl2FN3O 488.3 190-191 82 0.70
TQV(9) C29H21Cl2N3O 498.4 264-265 71 0.62
TQV(10) C29H22Cl2N4O 513.42 162-163 74 0.59
TQVI(1) C29H19Cl2N3O2S 544.4 180-181 60 0.60
TQVI(2) C29H18Cl3N3O2S 578.8 246-247 67 0.82
TQVI(3) C29H18Cl2N4O4S 589.4 212-213 64 0.79
TQVI(4) C29H19Cl2N3O3S 560.4 282-283 65 0.45
TQVI(5) C30H21Cl2N3O3S 574.4 270-271 67 0.50
TQVI(6) C32H25Cl2N3O5S 634.5 260-261 66 0.47
TQVI(7) C31H23Cl2N3O4S 604.5 220-221 61 0.52
TQVI(8) C29H18Cl2FN3O2S 562.4 230-231 74 0.80
TQVI(9) C31H23Cl2N3O2S 572.5 252-253 56 0.75
TQVI(10) C31H24Cl2N4O2S 587.52 196-197 67 0.48
7. Design, synthesis, characterization and biological evaluation of 3-(4-(7-chloro-2-(4-chlorophenyl)....
DOI: 10.9790/3008-10143036 www.iosrjournals.org 36 | Page
TQVI(6) 3,4,5-(OCH3)3- 17 22 20 23 16 13
TQVI(7) 3,4-(OCH3)2- 18 12 16 23 14 12
TQVI(8) 4-F- 18 15 19 20 08 14
TQVI(9) 4-CH2CH3 13 09 12 08 15 07
TQVI(10) 4-CH(CH3)2 12 9 18 17 16 15
DMFd
- - - - - - -
Ampicillin - 37 31 32 30
Amphotericin B - - - - - 18 17
a
Zone of inhibition in mm : Zone of inhibition of microbial growth around the cups in the agar medium,
measured in mm. b
Bacteria tested: Staphylococcus aureus (MTCC 3160) and Bacillus subtilis (MTCC 441).
Escherichia coli (MTCC 443) and Pseudomonas aeruginosa (MTCC 424).
c
Fungi tested : Aspergillus niger (MTCC 282) and Candida albicans (MTCC 227)
d
DMF: Dimethyl formamide.