1. The document describes the synthesis and characterization of new substituted 1,3,5-triazine compounds containing 1,2,4-triazole and substituted urea/thiourea groups.
2. These compounds were synthesized in a stepwise manner and characterized using techniques like IR, NMR and elemental analysis.
3. The antimicrobial activity of the synthesized compounds was evaluated against various microorganisms, with some compounds like 1c, 1e and 1g showing excellent activity.
Research Inventy : International Journal of Engineering and Scienceresearchinventy
Research Inventy : International Journal of Engineering and Science is published by the group of young academic and industrial researchers with 12 Issues per year. It is an online as well as print version open access journal that provides rapid publication (monthly) of articles in all areas of the subject such as: civil, mechanical, chemical, electronic and computer engineering as well as production and information technology. The Journal welcomes the submission of manuscripts that meet the general criteria of significance and scientific excellence. Papers will be published by rapid process within 20 days after acceptance and peer review process takes only 7 days. All articles published in Research Inventy will be peer-reviewed.
Synthesis, Identification and Surface Active Properties of Some Nonionic Surf...IOSRJAC
This research includes synthesis of new heterocyclic derivatives of quinazolinone and studying the possibility for their application as surfactants. The preparation process started by the reaction of pentadecanoyl chloride with anthranilic acid gave 2-pentadecyl-4H-benzo[3,1]oxazin-4-one [1] which was used as starting material to synthesis some heterocyclic compounds by a reaction with nitrogen nucleophiles. Compound [1] as starting material reacted by three ways. The first way react Compound [1] with semicarbazide, thiosemicarbazide and phenylsemicarbazide in pyridine as solvent to obtained [1-(4-oxo-2- pentadecylquinazolin-3(4H)-yl) urea [2], thiourea [3], phenylthiourea [4] respectively]. The second way include the reaction of Compound [1] with 99% hydrazine hydrate to produce 3-amino-2-pentadecylquinazolin- 4(3H)-one [5], then converted to amino derivatives [6-8] by the reaction of Compound [5] with different halogenated compounds such as (benzoyl chloride, acetyl chloride and chloro acetyl chloride ) in DMF and pyridine as catalyst. The third way include the reaction of compound [1] with different substituted amine and amide compounds (thiourea, hydroxylamine hydrochloride, glycine, ammonium acetate and phenyl hydrazine) respectively to obtain derivatives of quinazoline [9-14]. The produced compounds [2,4,5,7 and 12] react with propylene oxide in different moles (n=3, 5 and7) to yield novel groups of nonionic compounds having a function as surface active agents. The surface active properties like surface tension and interfacial tension, wetting time, cloud point, emulsion stability, foam height and CMC of these compounds were measured and showed a pronounced surface activity, good emulsifying properties and highly foaming in some of these compounds. Newly synthesized compounds were identified via spectral methods; their [FTIR and some of them by 1HNMR, 13C-NMR] and measurements of some of its physical properties.
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, Molecular Docking and Antimicrobial Evaluation of New Tetrahydrobe...ijtsrd
A series of novel derivatives of Tetrahydrobenzothienopyrimidine hydrazone were synthesized and product structure was elucidated by 1NMR, C13NMR and mass spectroscopy. The synthesized compounds were evaluated against fungal and bacterial strains. The synthesized compounds showed significant antibacterial activity against Staphylococcus aureus MTCC 96, Staphylococcus pyrogenes MTCC 442, and Escherichia coli MTCC 443, Pseudomonas aeruginosa MTCC 1688 and against fungal strains Candida albicans MTCC 227, Aspergillus niger MTCC 282, Aspergillus clavatus MTCC 1323. Some derivatives showed promising result against gram positive, gram negative bacterial and fungal strains than standard drug ampicillin and grieseofulvin. In- silico molecular docking studies of the synthesized compounds was done by using GRIP batch docking method of Vlife MDS 3.0 software to study their observed activity which showed a significant correlation between the binding score and biological activity for synthesized compounds. Neetu Chopra | Kiranpreet kaur | Sanjeev Kumar "Synthesis, Molecular Docking and Antimicrobial Evaluation of New Tetrahydrobenzothienopyrimidine Derivatives" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-2 | Issue-6 , October 2018, URL: http://www.ijtsrd.com/papers/ijtsrd18756.pdf
A optimized process for the synthesis of a key starting material for etodolac...IOSR Journals
Abstract An optimized process developed for the synthesis of 7-ethyltryptophol, a key starting material for etodolac, a non steroidal anti- inflammatory drug. Starting from commercially available 2-ethylphenylhydrazine. HCl and dihydro furan with con. H2SO4 as a catalyst in N, N- dimethyl acetamide ( DMAc). H2O (1:1) as a solvent in 75% yield . the method is easy, inexpensive , without purification getting pure solid. The process is very clean, high yielding & high quality and operationally simple.
Keywords: Etodolac, 7-ethyl tryptophol, 2-ethyl phenyl hydrazine hydrochloride, N,N-dimethyl acetamide.
Research Inventy : International Journal of Engineering and Scienceresearchinventy
Research Inventy : International Journal of Engineering and Science is published by the group of young academic and industrial researchers with 12 Issues per year. It is an online as well as print version open access journal that provides rapid publication (monthly) of articles in all areas of the subject such as: civil, mechanical, chemical, electronic and computer engineering as well as production and information technology. The Journal welcomes the submission of manuscripts that meet the general criteria of significance and scientific excellence. Papers will be published by rapid process within 20 days after acceptance and peer review process takes only 7 days. All articles published in Research Inventy will be peer-reviewed.
Synthesis, Identification and Surface Active Properties of Some Nonionic Surf...IOSRJAC
This research includes synthesis of new heterocyclic derivatives of quinazolinone and studying the possibility for their application as surfactants. The preparation process started by the reaction of pentadecanoyl chloride with anthranilic acid gave 2-pentadecyl-4H-benzo[3,1]oxazin-4-one [1] which was used as starting material to synthesis some heterocyclic compounds by a reaction with nitrogen nucleophiles. Compound [1] as starting material reacted by three ways. The first way react Compound [1] with semicarbazide, thiosemicarbazide and phenylsemicarbazide in pyridine as solvent to obtained [1-(4-oxo-2- pentadecylquinazolin-3(4H)-yl) urea [2], thiourea [3], phenylthiourea [4] respectively]. The second way include the reaction of Compound [1] with 99% hydrazine hydrate to produce 3-amino-2-pentadecylquinazolin- 4(3H)-one [5], then converted to amino derivatives [6-8] by the reaction of Compound [5] with different halogenated compounds such as (benzoyl chloride, acetyl chloride and chloro acetyl chloride ) in DMF and pyridine as catalyst. The third way include the reaction of compound [1] with different substituted amine and amide compounds (thiourea, hydroxylamine hydrochloride, glycine, ammonium acetate and phenyl hydrazine) respectively to obtain derivatives of quinazoline [9-14]. The produced compounds [2,4,5,7 and 12] react with propylene oxide in different moles (n=3, 5 and7) to yield novel groups of nonionic compounds having a function as surface active agents. The surface active properties like surface tension and interfacial tension, wetting time, cloud point, emulsion stability, foam height and CMC of these compounds were measured and showed a pronounced surface activity, good emulsifying properties and highly foaming in some of these compounds. Newly synthesized compounds were identified via spectral methods; their [FTIR and some of them by 1HNMR, 13C-NMR] and measurements of some of its physical properties.
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, Molecular Docking and Antimicrobial Evaluation of New Tetrahydrobe...ijtsrd
A series of novel derivatives of Tetrahydrobenzothienopyrimidine hydrazone were synthesized and product structure was elucidated by 1NMR, C13NMR and mass spectroscopy. The synthesized compounds were evaluated against fungal and bacterial strains. The synthesized compounds showed significant antibacterial activity against Staphylococcus aureus MTCC 96, Staphylococcus pyrogenes MTCC 442, and Escherichia coli MTCC 443, Pseudomonas aeruginosa MTCC 1688 and against fungal strains Candida albicans MTCC 227, Aspergillus niger MTCC 282, Aspergillus clavatus MTCC 1323. Some derivatives showed promising result against gram positive, gram negative bacterial and fungal strains than standard drug ampicillin and grieseofulvin. In- silico molecular docking studies of the synthesized compounds was done by using GRIP batch docking method of Vlife MDS 3.0 software to study their observed activity which showed a significant correlation between the binding score and biological activity for synthesized compounds. Neetu Chopra | Kiranpreet kaur | Sanjeev Kumar "Synthesis, Molecular Docking and Antimicrobial Evaluation of New Tetrahydrobenzothienopyrimidine Derivatives" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-2 | Issue-6 , October 2018, URL: http://www.ijtsrd.com/papers/ijtsrd18756.pdf
A optimized process for the synthesis of a key starting material for etodolac...IOSR Journals
Abstract An optimized process developed for the synthesis of 7-ethyltryptophol, a key starting material for etodolac, a non steroidal anti- inflammatory drug. Starting from commercially available 2-ethylphenylhydrazine. HCl and dihydro furan with con. H2SO4 as a catalyst in N, N- dimethyl acetamide ( DMAc). H2O (1:1) as a solvent in 75% yield . the method is easy, inexpensive , without purification getting pure solid. The process is very clean, high yielding & high quality and operationally simple.
Keywords: Etodolac, 7-ethyl tryptophol, 2-ethyl phenyl hydrazine hydrochloride, N,N-dimethyl acetamide.
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 Evaluation of Some Nitro-Mannich Bases Derived fr...peertechzpublication
The present work focused on exploring the reactivity of β-nitrostyrene towards Mannich reaction
with different approaches. The synthesized nitro-Mannich bases were tested as antimicrobial agents
that showed high activity against both gram positive and gram negative bacteria.
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 Pharmacological evaluation of new Benzoxozole DerivativesSriramNagarajan15
Benzoxazoles1 are usually prepared by heating 2-Aminophenol with formic acids in the presence of Boric acid under reflux. Condensation of these two substances under milder conditions. Being a heterocyclic compound, benzoxazole finds use in research as a starting material for the synthesis of larger, usually bioactive structures. It is found within the chemical structures of pharmaceutical drugs such as flunoxaprofen. Benzoxazole derivatives are provided a protection against noxious UV radiation.Benzoxazole derivatives are also used in cosmotic compositions, such as for examples mainly cinnamic acid, 4-aminobenzoic acid.Benzoxazole derivatives are also used in the optical brighteners.These derivatives are used as Anticonvulsant and Neurotoxicity2 , Anti-inflammatory agents3, “Antibacterial activity”4, Cholesteryl ester transfer Protein inhibitors5, Antimicrobial activity6,7, Antifungal activity’8, Cyclooxygenase inhibitors9, hair treatment products and also used as a skin protectants.
Mixed Ligand, Palladium(II) and Platinum(II) Complexes of Tertiary Diphosphin...Karwan Omer
Palladium(II) and platinum(II) complexes containing the mixed ligands tertiary
diphosphinesdppm. dppp and dppf with Thioester ligand S-1H benzo[d] imidazole-2-yl benzothioate
(HSBIBT) have been prepared by the reaction of PdCl2 and PtCl2 with one equiv of tertiary
diphosphines ligands to form [Pd(k2-dppf)Cl2], [Pd(k2-dppp)Cl2] and [Pt(k2-dppmCl)Cl2] complexes
and then add the ligand HSBIBT to these complexes to form mixed ligand complexes. The prepared
complexes have been characterized by single-crystal X-ray diffraction, elemental analysis, magnetic
susceptibility, molar conductance, IR spectral data and UV-Visible. The results suggested that the
ligand HSBIBT bonded to the metal through N atom and square planner geometries were assigned
for the complexes.
Design, Synthesis, Biological Evaluation, and In Silico ADMET Studies of 1,8-...BRNSS Publication Hub
In the present study, 1,8-naphthyridine-3-carboxylic acid derivatives (5a1, 5a2, 5b1, and 5b2) were
designed, synthesized, and screened for their in vitro H1-antihistaminic activity. H1R inhibitory activity
of the synthesized derivatives was calculated by the modified Van Arman technique, histamine-induced
bronchoconstriction in guinea pigs. A good bronchorelaxant effect of compounds was observed in
histamine-contracted guinea pig tracheal chain through H1-receptor antagonism. In addition, the
hypothetically resulted compounds are checked for their reliability on other in silico drug designing
online web services like SwissADME predictor. In silico ADMET analysis results show that all the
derivatives had negligible toxicity, good absorption, and solubility profile. These compounds may serve
as possible lead for establishing safe and effective antihistaminic agent(s).
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
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.
Phytochemical screening and in vitro antioxidant activity of extracts of jasm...SriramNagarajan16
Objectives
The aims of this research were to carry out the preliminary phytochemical screening and antioxidant activity
of different extracts of J. sessiliflorum. The different anti-oxidant methods carried out were DPPH
scavenging method, NBT dye reduction method and nitric oxide scavenging method
Methods
Extracts were prepared by reflux method using different polarity solvents. The extracts were evap orated
using rotary evaporator. Antioxidant activities using DPPH, NBT dye reduction method and nitric oxide
scavenging methods and the correlation of their IC50 values with standards were carried out.
Results
The ethanolic herbs extract of J. sessiliflorum had the lowest IC50 values in all the anti-oxidant methods.
Moreover, the ethanolic extracts showed the presence greatest amount of phytochemical constituents. The
IC50 values were correlated with the IC50 values of standards in all the anti- oxidant activity determination
methods.
Conclusions
The results of the present study indicate that the extracts of J.sessiliflorum exhibited strong antioxidant
activity and thus it is a good source of antioxidant.
Ninhydrin Based Visible Spectrophotometric Determination of GemigliptinRatnakaram Venkata Nadh
A simple method is described to determine the amount of gemigliptin in bulk and tablet formulation by visible spectrophotometry. Basis of the proposed method is the reaction of the primary amine present on gemigliptin with ninhydrin in alkaline pH (alkaline borate buffer) medium to produce a purple color (Ruhemann’s purple) which has maximum absorption at 558 nm. The method was validated as per the current ICH guidelines. The obtained regression equation (y = 0.0148x+0.0011) in the range of 5-30 μg mL-1 has a good correlation coefficient (> 0.999). As the method does not require any separation, it is rapid and simple. The recovery levels of the drug were in the range of 99.73 – 99.96. This method is a green method as it no organic solvents were employed
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,
Synthesis and Characterization of a New Cationic Surfactant Derived from 5-Ch...IJERA Editor
:In this paper, anovel cationic surfactant is synthesized by the alkylation reaction of 5-Chloro- 1H-indole-2,3-dioneunder the conditions of phase transfer catalysis and quaternizationby trimethylamine in acetone solution.Chemical structures of synthesized compounds were confirmed by 1HNMR and 13C NMR. The micellization of cationic surfactant in aqueous solution at room temperature has been reported using the conductivity of the measurements
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.
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 Evaluation of Some Nitro-Mannich Bases Derived fr...peertechzpublication
The present work focused on exploring the reactivity of β-nitrostyrene towards Mannich reaction
with different approaches. The synthesized nitro-Mannich bases were tested as antimicrobial agents
that showed high activity against both gram positive and gram negative bacteria.
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 Pharmacological evaluation of new Benzoxozole DerivativesSriramNagarajan15
Benzoxazoles1 are usually prepared by heating 2-Aminophenol with formic acids in the presence of Boric acid under reflux. Condensation of these two substances under milder conditions. Being a heterocyclic compound, benzoxazole finds use in research as a starting material for the synthesis of larger, usually bioactive structures. It is found within the chemical structures of pharmaceutical drugs such as flunoxaprofen. Benzoxazole derivatives are provided a protection against noxious UV radiation.Benzoxazole derivatives are also used in cosmotic compositions, such as for examples mainly cinnamic acid, 4-aminobenzoic acid.Benzoxazole derivatives are also used in the optical brighteners.These derivatives are used as Anticonvulsant and Neurotoxicity2 , Anti-inflammatory agents3, “Antibacterial activity”4, Cholesteryl ester transfer Protein inhibitors5, Antimicrobial activity6,7, Antifungal activity’8, Cyclooxygenase inhibitors9, hair treatment products and also used as a skin protectants.
Mixed Ligand, Palladium(II) and Platinum(II) Complexes of Tertiary Diphosphin...Karwan Omer
Palladium(II) and platinum(II) complexes containing the mixed ligands tertiary
diphosphinesdppm. dppp and dppf with Thioester ligand S-1H benzo[d] imidazole-2-yl benzothioate
(HSBIBT) have been prepared by the reaction of PdCl2 and PtCl2 with one equiv of tertiary
diphosphines ligands to form [Pd(k2-dppf)Cl2], [Pd(k2-dppp)Cl2] and [Pt(k2-dppmCl)Cl2] complexes
and then add the ligand HSBIBT to these complexes to form mixed ligand complexes. The prepared
complexes have been characterized by single-crystal X-ray diffraction, elemental analysis, magnetic
susceptibility, molar conductance, IR spectral data and UV-Visible. The results suggested that the
ligand HSBIBT bonded to the metal through N atom and square planner geometries were assigned
for the complexes.
Design, Synthesis, Biological Evaluation, and In Silico ADMET Studies of 1,8-...BRNSS Publication Hub
In the present study, 1,8-naphthyridine-3-carboxylic acid derivatives (5a1, 5a2, 5b1, and 5b2) were
designed, synthesized, and screened for their in vitro H1-antihistaminic activity. H1R inhibitory activity
of the synthesized derivatives was calculated by the modified Van Arman technique, histamine-induced
bronchoconstriction in guinea pigs. A good bronchorelaxant effect of compounds was observed in
histamine-contracted guinea pig tracheal chain through H1-receptor antagonism. In addition, the
hypothetically resulted compounds are checked for their reliability on other in silico drug designing
online web services like SwissADME predictor. In silico ADMET analysis results show that all the
derivatives had negligible toxicity, good absorption, and solubility profile. These compounds may serve
as possible lead for establishing safe and effective antihistaminic agent(s).
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
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.
Phytochemical screening and in vitro antioxidant activity of extracts of jasm...SriramNagarajan16
Objectives
The aims of this research were to carry out the preliminary phytochemical screening and antioxidant activity
of different extracts of J. sessiliflorum. The different anti-oxidant methods carried out were DPPH
scavenging method, NBT dye reduction method and nitric oxide scavenging method
Methods
Extracts were prepared by reflux method using different polarity solvents. The extracts were evap orated
using rotary evaporator. Antioxidant activities using DPPH, NBT dye reduction method and nitric oxide
scavenging methods and the correlation of their IC50 values with standards were carried out.
Results
The ethanolic herbs extract of J. sessiliflorum had the lowest IC50 values in all the anti-oxidant methods.
Moreover, the ethanolic extracts showed the presence greatest amount of phytochemical constituents. The
IC50 values were correlated with the IC50 values of standards in all the anti- oxidant activity determination
methods.
Conclusions
The results of the present study indicate that the extracts of J.sessiliflorum exhibited strong antioxidant
activity and thus it is a good source of antioxidant.
Ninhydrin Based Visible Spectrophotometric Determination of GemigliptinRatnakaram Venkata Nadh
A simple method is described to determine the amount of gemigliptin in bulk and tablet formulation by visible spectrophotometry. Basis of the proposed method is the reaction of the primary amine present on gemigliptin with ninhydrin in alkaline pH (alkaline borate buffer) medium to produce a purple color (Ruhemann’s purple) which has maximum absorption at 558 nm. The method was validated as per the current ICH guidelines. The obtained regression equation (y = 0.0148x+0.0011) in the range of 5-30 μg mL-1 has a good correlation coefficient (> 0.999). As the method does not require any separation, it is rapid and simple. The recovery levels of the drug were in the range of 99.73 – 99.96. This method is a green method as it no organic solvents were employed
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,
Synthesis and Characterization of a New Cationic Surfactant Derived from 5-Ch...IJERA Editor
:In this paper, anovel cationic surfactant is synthesized by the alkylation reaction of 5-Chloro- 1H-indole-2,3-dioneunder the conditions of phase transfer catalysis and quaternizationby trimethylamine in acetone solution.Chemical structures of synthesized compounds were confirmed by 1HNMR and 13C NMR. The micellization of cationic surfactant in aqueous solution at room temperature has been reported using the conductivity of the measurements
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.
A presentation I gave on the methodology of my thesis project at ITP. The details of the system (ie, the use of Nintendo DSes and/or Socialbomb hardware) were just for reference, as the final implementation will likely be quite different. Including that example, though, seems to have been the thing that makes what I'm after clearer to people, so I'm glad I included it, despite my reservations about discussing platforms that I'm not using.
There's also a rather thorough description of a card game prototype I developed to test some of the rules and ideas I've been working on for alliances. I think you can even play it based on what's in the presentation! If you do, please let me know!
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.
Physical and Structural Characterization of Biofield Treated Imidazole Deriva...albertdivis
The Aim of present study was to evaluate the impact of biofield treatment on two imidazole derivatives (i.e., imidazole and 2-methylimidazole) by various analytical methods.
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.
Assessment of Antimicrobial, Anti-Inflammatory Activity and Docking Study of ...ijtsrd
A novel series of 2- arylimino -5- indole-2-yl-methylidene -1,3-thiazolidine-4-onederivatives were synthesized and screened for their anti-inflammatory and analgesic potential. The structures of newly synthesized compounds were confirmed by their analytical and spectroscopic data using IR and 1H-NMR. The novel compounds were evaluated for their anti-inflammatory potential using carrageenan induced paw edema model and analgesic activity using acetic acid induced abdominal writhing test. Three compounds 4g,4m and 4o alleviated inflammation more than the standard drug Diclofenac Sodium. The synthesized compounds also showed significant analgesic activity. In-silicomoleculardocking studies of the synthesized compounds were done on crystal structure of Cyclooxygenase-2using Glide version 5.0 following the standard procedure recommended by Schrodinger to study their observed activity, which revealed a significant correlation between the binding score and biological activity for these compounds. Maximum Glide score was obtained for compound 4o having a value of -7.42. This compound showed one interaction with the enzyme. Neetu Chopra | Kiranpreet Kaur | Sandeep Kaur "Assessment of Antimicrobial, Anti-Inflammatory Activity and Docking Study of Novel 2-(Arylimino)-5-(Indole-2-Yl-Methylidene)-1, 3-Thiazolidine-4-one Derivatives" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-2 | Issue-6 , October 2018, URL: http://www.ijtsrd.com/papers/ijtsrd18822.pdf
A STUDY TO EVALUATE THE IN VITRO ANTIMICROBIAL ACTIVITY AND ANTIANDROGENIC E...Dr. Pradeep mitharwal
The present paper deals with synthesis and characterization
of some new chromium (III) Schiff base complexes using microwave irradiation
technique as well as conventional heating. The S∩N donor benzothiazolines, 1-
(2-furanyl) ethanone benzothiazoline (Bzt1N
∩
SH), 1-(2-thienyl) ethanone
benzothiazoline (Bzt2N
∩
SH) and 1-(2-pyridyl) ethanone benzothiazoline
(Bzt3N
∩
SH) were prepared by the condensation of ortho-aminothiophenol with
respective ketones in ethanol.
A series of novel 5-[2-(4-fluorobenzyl)-6-aryl-imidazo[2,1-b][1,3,4]thiadiazol-5-ylmethylene] thiazolidine-2,4-dione derivatives (4a-d) were synthesized. These final compounds (4a-d) were synthesized by Knoevenagel condensation of 2-(4-fluorobenzyl)-6-arylimidazo[2,1-b][1,3,4]thiadiazole-5-carbaldehydes (3a-d) with thiazolidine-2,4-dione. All the newly synthesized compounds were screened for their invivo hypoglycemic and hypolipidemic activity in male Wister rats. The Structures of all the newly synthesized compounds were established by analytical and spectral data.
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
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.
In vitro enzyme inhibition studies on new sulfonamide derivatives of 4-tosyl ...Jing Zang
Sulfonamides are considered to be pharmaceutically important class of compounds. In the present work, N-(2,4-dimethylphenyl)-4-toluenesulfonamide (3) was synthesized by the reaction of 2,4-dimethylaniline (1) and 4-tosyl chloride (2; 4-methylbenzenesulfonyl chloride) using 10% aqueous Na2CO3 solution as reaction medium. At the second step, the synthesized molecule 3 was made to react with different alkyl/aralkyl halides (4a-o) to yield the target compounds, 5a-o, using N,N-dimethylformamide (DMF) as reaction medium and lithium hydride as an activator. The synthesis of all the compounds was verified by spectral techniques using IR, 1H-NMR and EIMS; and further examined for their anti-enzymatic activities. The synthesized compound 5f represented a suitable inhibitory potential against α-glucosidase and lipoxygenase enzymes.
Biofield Treatment Impact on 1,2,4-Triazoledeeptimishra10
The biofield treatment has improved the growth and production of agriculture crops and significantly altered the phenotypic characteristics of various pathogenic microbes. Additionally, biofield treatment has substantially altered the medicinal, growth and anatomical properties of ashwagandha.
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GDG Cloud Southlake #33: Boule & Rebala: Effective AppSec in SDLC using Deplo...James Anderson
Effective Application Security in Software Delivery lifecycle using Deployment Firewall and DBOM
The modern software delivery process (or the CI/CD process) includes many tools, distributed teams, open-source code, and cloud platforms. Constant focus on speed to release software to market, along with the traditional slow and manual security checks has caused gaps in continuous security as an important piece in the software supply chain. Today organizations feel more susceptible to external and internal cyber threats due to the vast attack surface in their applications supply chain and the lack of end-to-end governance and risk management.
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Threats to mobile devices are more prevalent and increasing in scope and complexity. Users of mobile devices desire to take full advantage of the features
available on those devices, but many of the features provide convenience and capability but sacrifice security. This best practices guide outlines steps the users can take to better protect personal devices and information.
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Observability Concepts EVERY Developer Should Know -- DeveloperWeek Europe.pdfPaige Cruz
Monitoring and observability aren’t traditionally found in software curriculums and many of us cobble this knowledge together from whatever vendor or ecosystem we were first introduced to and whatever is a part of your current company’s observability stack.
While the dev and ops silo continues to crumble….many organizations still relegate monitoring & observability as the purview of ops, infra and SRE teams. This is a mistake - achieving a highly observable system requires collaboration up and down the stack.
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In the rapidly evolving landscape of technologies, XML continues to play a vital role in structuring, storing, and transporting data across diverse systems. The recent advancements in artificial intelligence (AI) present new methodologies for enhancing XML development workflows, introducing efficiency, automation, and intelligent capabilities. This presentation will outline the scope and perspective of utilizing AI in XML development. The potential benefits and the possible pitfalls will be highlighted, providing a balanced view of the subject.
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Welcome to UiPath Test Automation using UiPath Test Suite series part 6. In this session, we will cover Test Automation with generative AI and Open AI.
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20240609 QFM020 Irresponsible AI Reading List May 2024
Synthesis, characterization, antimicrobial
1. Chemistry and Materials Research www.iiste.org
ISSN 2224- 3224 (Print) ISSN 2225- 0956 (Online)
Vol 1, No.2, 2011
Synthesis, Characterization, Antimicrobial
Studies of Certain Triazole Containing
S-Triazine Derived Compound
Dr.Kokila N. Sarmah*, Talha V.Patel.
*Selection Grade Lecturer, Department of chemistry,
Shree Jayendrapuri Arts & Science College, Bharuch-392002.
Research Student under the guidance of Dr. Kokila N. Sarmah.
Worked at Shree Jayendrapuri Arts & Science College, Bharuch.
Gujarat, India-392002.
talha.patel9@gmail.com
Abstract
Some new substituted 1,3,5 triazine with 1,2,4 triazole and substituted urea/thiourea were synthesized and
evaluated for their in vitro antimicrobial activity against Gram positive and Gram negative strains using a
-1
microdilution procedure. Synthesized compounds 1a to 1i prove to be effective with MIC (mg ml ), among
them 1c, 1e, 1g showed excellent activity against a panel of microorganisms. The newly synthesized
1
compounds were characterized using IR, H-NMR and elemental analysis.
Keywords :- 1,2,4 Triazole, Substituted urea/thiourea, Cyanuric chloride and Antimicrobial activity.
Introduction:-
s-Triazine derivatives represent an important class of compounds due to their potential to be biologically active.
They are known to be anti-protozoals[1], anticancer agents[2], estrogen receptor modulators[3], antimalarials[4],
cyclin-dependent kinase modulators[5], and antimicrobials[6]. Cyanuric chloride, an inexpensive, easily available
reagent, of low toxicity and less corrosive than other similar reactants, has been widely used in organic
reactions[7]. In the present research, we wish to describe a simple and efficient protocol for the rapid preparation
of 1-(4-(3-(4-METHOXYPHENYL)THIOUREIDO)-6-(1H-1,2,4-TRIAZOL-1-YL)-1,3,5-TRIAZINE-2-YL)-
3-PHENYLUREA at different temperature conditions. To the best of our knowledge, there are no reports on
three-component coupling of triazole, substituted urea and thiourea to produce a title compound. An important
class of compounds having anticancer, antitumor, antiviral and antifungal activity consists of substituted s-
triazine
derivatives. These compounds have been used in the treatment of depression and hence gained considerable
significance. These are valuable bases for estrogen receptor modulators [8] and also used as bridging agents to
synthesize herbicides and in the production of drugs or polymers[9].
1,3,5-Triazine derivatives[10]have displayed a broad range of biological activities including cytotoxic
activities[11-13], antiangiogenic activity by targeting either VEGF-R2 (KDR)[14]or direct modulation of Tie-2
tyrosine kinase phosphorylation[15], antiparasitic activities[16,17], and glucocerebrosidase inhibition with potential
as chemical chaperones for Gaucher disease[18]. Cyanuric chloride derivatives have been studied for decades,
especially its amino derivatives. It is generally accepted that the first chlorine of cyanuric chloride can be easily
1
2. Chemistry and Materials Research www.iiste.org
ISSN 2224- 3224 (Print) ISSN 2225- 0956 (Online)
Vol 1, No.2, 2011
substituted by NH2-group at 0–5 ◦C, the second one at 30–50 ◦C, and the third one typically above 80 ◦C, which
depends on the activity of amine nucleophiles[19].
1,2,4 – Triazole have wide range of biological activities such as anti bacterial[20] , anti caner[21] , anti
tubercular[22], anti HIV[23] and anti depressant activity, anti tumer [24] and anti viral[24] activity, anti
hypertensive[25] activity , analgesic and anti inflammatory[26] activity.
[27]
Thiourea derivatives possess antibacterial , hypnotic antitubercular and possible anticonvulsant
activities. It also represent a new class of human immuno deficiency virus type (HIV-1), non-nucleoside
[28] [29]
reverse transcriptase (NNRT) inhibitors , found as antagonist , and high density lipoprotein (HDL)
[30]
elevating agents . Over the last few years, the thiourea moiety has been of interest to design molecules as
receptor antagonists, as natural product mimics or as synthetic intermediates to amidines or guanidines.[31]
Thiourea not only confers antibacterial, antitubercular or antileprotic activity, but has also been reported to
possess antifungal as well as antiviral properties.[32]
Urea derivatives are reported to possess antibacterial[33], antimicrobial antifungal, anticancer[34] and
anticonvulsant[35] activities. Urea derivatives possess wide therapeutic activities such as antithyroidal[36],
hypnotic and anesthetic[37], antibacterial[38], diuretic[39] and anthelmintics.
We planned to undertake the synthesis and characterization of some triazine derivatives carrying the above
biodynamic heterocyclic systems with the hope to achieve enhanced biological activity.
Experimental:-
General
All the melting points were taken in open capillaries tube and are uncorrected. The purity of compounds was
checked routinely by TLC (0.5 mm thickness)Using silica gel – G coated Al – plates (Merck) and spots were
visualized by exposing the dry plates in iodine vapours. IR spectra were recorded on FTIR spectrophotometer
using KBr or Nujol technique.1H NMR spectra on a Varian 400 FT MHz NMR instrument at using CDCl3 or
DMSO-d6 as solvent and TMS as internal reference.
Scheme:-
STEP-1
PREPARATION OF 1-(4,6-DICHLORO-1,3,5-TRIAZIN-2-YL)-3-(4-
METHOXYPHENYL)THIOUREA: (A)
To a stirred solution of cyanuric chloride (0.1 mole, 18.4 g.) in acetone (100 ml) at 0-50C, the solution of 1–(4-
methoxyphenyl)thiourea (0.1 mole,17.3g) in acetone (45 ml) was added and pH being maintained neutral by
the addition of 10% sodium bi-carbonate solution from time to time as per requirement of reaction condition.
The stirring was continued at 0-5°C for 2 hours. After the completion of reaction the stirring was stopped and
the solution was treated with crushed ice. The solid product obtained was filtered and dried. The crude product
was purified by crystallization from absolute alcohol to get title compound.
STEP-2
PREPARATION OF 1-(4-CHLORO-6-(1 H-1,2,4-TRIAZOL-1-YL)-1,3,5-TRIAZINE-2-YL)-3-(4-
METHOXYPHENYL) THIOUREA : (B)
2
3. Chemistry and Materials Research www.iiste.org
ISSN 2224- 3224 (Print) ISSN 2225- 0956 (Online)
Vol 1, No.2, 2011
To a stirred solution of (A) (0.1 mole, 33.0 g) in acetone (100 ml) was added, the solution of 1,2,4 triazole (0.1
mole, 6.9 g ) in acetone (25 ml) was added drop wise maintaining the temperature at 40°C, the pH being
maintained neutral by the addition of 10% sodium bi-carbonate solution from time to time as per requirement of
reaction condition. The temperature was gradually raised to 45°C during three hours. After the completion of
reaction, the resultant content was poured into ice-cold water. The solid product obtained was filtered and dried.
The crude product was purified by crystallization from absolute alcohol to get the title compound.
STEP-3
PREPARATION OF FINAL COMPOUND:-
A mixture of (B) (0.01 mole, 3.62 g) and aryl urea (0.01 mole) in DMF (20ml) was refluxed in oil bath. The
temperature was gradually raised to 80-1000C during four hours, the pH being maintained neutral by the
addition of 10% sodium bi-carbonate solution from time to time as per requirement of reaction condition. After
the completion of reaction, add little charcoal in R.B.F. and then filter it into cold water. The solid product
obtained was filtered and dried. The crude product was purified by recrystallization from absolute alcohol.
Prepare all derivatives by this method. Analytical data are given below.
ROUTE OF SYNTHESIS :-
STEP-1
[A]
STEP-2
3
4. Chemistry and Materials Research www.iiste.org
ISSN 2224- 3224 (Print) ISSN 2225- 0956 (Online)
Vol 1, No.2, 2011
[B]
STEP-3
WHERE R = given in below table.
Table 1 Physical data of synthesized compounds:-
Sr. No. R Mol. Yield
Mol. Formula M.P. OC
Weight %
1a H C20H18N10O2S 462.49 120O 60
1b 2-OCH3 C21H20N10O3S 492.51 122 O 61
1c 4-CH3 C21H20N10O2S 476.51 190 O 59
O
1d 4-Cl C20H17ClN10O2S 496.93 220 74
O
1e 4-OCH3 C21H20N10O3S 492.51 140 59
O
1f 2-CH3 C21H20N10O2S 476.51 140 58
1g 2-Cl C20H17ClN10O2S 496.93 135 O 62
O
1h 4-Br C20H17BrN10O2S 541.38 180 60
O
1i 4-F C20H17FN10O2S 480.48 175 65
4
6. Chemistry and Materials Research www.iiste.org
ISSN 2224- 3224 (Print) ISSN 2225- 0956 (Online)
Vol 1, No.2, 2011
Sr.No µ
Minimum Inhibitory Concentration (µg/ml)
&
Compound (1g): Yield: 62%; m.p. 1350C (dec.); IR (KBr,cm-1) : 789.30 cm-1
(-C=N- s-triazine) 825.30 cm-1(1,4 Di sub. in benzene) 1430.10 cm-1(>N-,30 amine)1565.60 cm-1(-NH-
def)1650.70 cm-1 (-C=O-) 3310.80 cm-1(-NH-str)2900.50 cm-1 (–OCH3 str)1170.60cm-1(-C=S-)717 cm-1(-C-Cl-
str)1036.74 cm-1 (-N-N-str) 1H-NMR:δ 8.70(s,2H,-CONH) 10.29(s,2H,-CSNH),3.75(s,3H, -OCH3)7.50-7.84
(m,10H, Ar-H).
Compound (1h): Yield: 60%; m.p. 1800C (dec.); IR (KBr,cm-1) : 797.40 cm-1 (-C=N- s-triazine) 829.90 cm-
1
(1,4 Di sub. in benzene) 1420.10 cm-1(>N-,30 amine)1560.50cm-1 (-NH-def)1654.90 cm-1 (-C=O-) 33170.55
cm-1(-NH-str)2920.45 cm-1 (–OCH3 str) 1162.70cm-1(-C=S-)692 cm-1(-C-Br-str) 1028.47 cm-1 (-N-N-str) 1H-
NMR:δ 8.67(s,2H,-CONH) 10.75(s,2H,-CSNH),3.66(s,3H,-OCH3)7.42-7.74(m,10H, Ar-H).
Compound (1i): Yield: 65%; m.p. 1750C (dec.); IR (KBr,cm-1) : 790.30 cm-1
(-C=N- s-triazine) 820.40 cm-1(1,4 Di sub. in benzene) 1435.10 cm-1(>N-,30 amine)1561.50 cm-1(-NH-
def)1642.60 cm-1 (-C=O-) 3300.75 cm-1(-NH-str)2914.50 cm-1
(–OCH3 str)1160.60cm-1(-C=S-)1055 cm-1(-C-F-str) 1040.10 cm-1 (-N-N-str) 1H-NMR:δ 8.75(s,2H,-CONH)
10.40(s,2H,-CSNH),3.85(s,3H, -OCH3)7.70-7.94 (m,10H, Ar-H).
Antimicrobial Activity
For the testing antimicrobial activity various microorganism were used for the study. The broth dilution
method was used for this study. Following general procedure is adopted[40].The antimicrobial activity of all the
compounds was studies at 1000 ppm concentration in vitro. The different types of microorganism used were
some gram negative bacteria [Escherichia coli, Pseudomonas aeruginosa], gram positive bacteria [Bacillus
subtilis, Staphylococcus aureus] and fungus [Candida albicans].
µ
80% DMSO are used as solvent to dissolve compound 1a to 1i to 10(µg/ml).
Conclusions:-
A series of cyanuric chloride derivatives were prepared and tested for their in vitro antibacterial activity against
the four strains of bacteria (gram +ve, gram –ve).Three compounds of the obtained series showed high in vitro
antimicrobial activity. Compound (1c,1e,1g) showed excellent activity against Staphylococcus aureus. Whereas
compound 1c has excellent activity against B. subtilis, P. aeruginosa, C. albicans.
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Gram positive bacteria Gram negative bacteria Fungus
R S. aureus B. subtilis E. coli P. aeruginosa C. albicans
1. 1a H 125-250 250-500 125-250 125-250 125-250
2. 1b 2-OCH3 125-250 125-250 125-250 250-500 125-250
3. 1c 4-CH3 125-250 31.25-62.5 125-250 31.25-62.5 31.25-62.5
4. 1d 4-Cl 125-250 250-500 125-250 125-250 125-250
5. 1e 4-OCH3 62.5-125 125-250 125-250 125-250 125-250
6. 1f 2-CH3 125-250 125-250 125-250 125-250 125-250
7. 1g 2-Cl 62.5-125 125-250 125-250 125-250 250-500
8. 1h 4-Br 125-250 125-250 125-250 125-250 250-500
9. 1i 4-F 125-250 125-250 125-250 125-250 125-250
Ampicillin ------ 250 100 100 100 ------
Nystatin ------ --- --- --- --- 100
Note: The higher value in given range is MIC but practically we can find out exact value from the given range
by using different dilutions.(by secondary screening).
Acknowledgements:-
The authors are thankful to the Head of the Chemistry Department, Dr.N.M.Patel and Dr.M.P.Peerzada, Shree
jayendrapuri Arts & Science College, Bharuch.The authors also express their sincere thanks to the COE, Vapi
for spectral analysis and Advance laboratory,bharuch for giving facility to work antimicrobial screening.
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