Pub Date : 2019-10-12DOI: 10.14233/ajomc.2019.ajomc-p211
D. Pandya, Y. Naliapara
We report a novel methodology for the efficient and rapid synthesis of core intermediate 2-(2H-1,2,3- triazol-2-yl)benzoic acid using trans-N,N’-dimethylcyclohexane-1,2-diamine as a catalyst and copper iodide as co-catalyst under microwave irradiations and a series of novel N-phenyl-2-(2H-1,2,3-triazol- 2-yl)benzamide derivatives via acid-amine coupling reaction using DCC as a dehydrating agent and DMAP as a base. In comparison to the conventional heating procedure and performing the reaction using different combinations of catalysts and bases, the time of synthesis and efforts are significantly reduced in the present method, which also gave excellent yield. The scaffold and all novel amides were characterized by spectroscopic techniques.
{"title":"Microwave-Assisted C-N Coupling for the Synthesis of 2-(2H-1,2,3-Triazol-2-yl)benzoic\u0000Acid Scaffold and Novel N-Phenyl-2-(2H-1,2,3-triazol-2-yl)benzamide Derivatives","authors":"D. Pandya, Y. Naliapara","doi":"10.14233/ajomc.2019.ajomc-p211","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p211","url":null,"abstract":"We report a novel methodology for the efficient and rapid synthesis of core intermediate 2-(2H-1,2,3-\u0000triazol-2-yl)benzoic acid using trans-N,N’-dimethylcyclohexane-1,2-diamine as a catalyst and copper\u0000iodide as co-catalyst under microwave irradiations and a series of novel N-phenyl-2-(2H-1,2,3-triazol-\u00002-yl)benzamide derivatives via acid-amine coupling reaction using DCC as a dehydrating agent and\u0000DMAP as a base. In comparison to the conventional heating procedure and performing the reaction\u0000using different combinations of catalysts and bases, the time of synthesis and efforts are significantly\u0000reduced in the present method, which also gave excellent yield. The scaffold and all novel amides\u0000were characterized by spectroscopic techniques.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"113 5-6 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80222801","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-10-12DOI: 10.14233/ajomc.2019.ajomc-p172
R. Ukirde, R. Patil, S. D. Sawant
Coumarin derivatives are an important class of heterocyclic compounds, specifically 4-amino substituted coumarins with antioxidant, anticancer activities. The above observations prompted us to synthesize new coumarins with various substitutions. The starting material 4-chloro-2H-chromen-2-one was synthesized by refluxing a mixture of 4-hydroxy-2H-chromen-2-one in phosphoryl chloride. The 4-substituted amine derivatives of coumarin were synthesized by refluxing 4-chloro-2H-chromen-2- one with 4-substituted amines and anhydrous K2CO3 and methanol. All the eleven 4-substituted amine derivatives of coumarin were synthesized by replacing chloro group with different amines. These coumarin derivatives were evaluated for in vitro antioxidant activity using quercetin as standard.
{"title":"Design, Synthesis and Evaluation of Antioxidant Activity of Some Coumarin Derivatives","authors":"R. Ukirde, R. Patil, S. D. Sawant","doi":"10.14233/ajomc.2019.ajomc-p172","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p172","url":null,"abstract":"Coumarin derivatives are an important class of heterocyclic compounds, specifically 4-amino substituted\u0000coumarins with antioxidant, anticancer activities. The above observations prompted us to synthesize\u0000new coumarins with various substitutions. The starting material 4-chloro-2H-chromen-2-one was\u0000synthesized by refluxing a mixture of 4-hydroxy-2H-chromen-2-one in phosphoryl chloride. The\u00004-substituted amine derivatives of coumarin were synthesized by refluxing 4-chloro-2H-chromen-2-\u0000one with 4-substituted amines and anhydrous K2CO3 and methanol. All the eleven 4-substituted amine\u0000derivatives of coumarin were synthesized by replacing chloro group with different amines. These\u0000coumarin derivatives were evaluated for in vitro antioxidant activity using quercetin as standard.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"75 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73003234","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-10-12DOI: 10.14233/ajomc.2019.ajomc-p217
Vijetha Pendyala, V. Suryadevara, Subbarao Jampani, Suhasini Jala
Present study was an attempt to investigate the bioactive components present in the leaves of Guaiacum officinale using gas chromatography-mass spectroscopy (GC-MS) analysis and study the antiinflammatory potential of those constituents using molecular docking studies. GC-MS analysis was done by standard protocol using the equipment JEOL GC MATE II. The identification of components was based on NIST (National Institute of Standards and Technology) Version-11 library as well as comparison of their retention indices. The molecular docking studies were done using the commercial docking software MCULE, 1-click docking. GC-MS analysis of the alcoholic extract showed the presence of ten compounds at different retention times. The phytoconstituent 8,11,14-eicosatrienoic acid was present at high concentration with % peak area of 43.3 at a retention time of 19.43 min followed by 5,7-dihydroxy-8-methoxy flavone (Wogonin) at a retention time of 17.73. All 10 compounds obtained from GC-MS analysis and diclofenac were used as the ligands in this study, with cyclooxygenase-2 (COX-2), phospholipase A2 and interleukin receptor as the molecular targets. in silico Docking studies revealed that the flavanoid Wogonin is having highest binding potential indicated by least docking score of -8.2, -8 and -6.9 kcal/mol on COX-2, phospholipase A2 and interleukin receptor respectively.
{"title":"GC-MS Analysis and Molecular Docking of Bioactive Components from\u0000Leaves of Guaiacum officinale for Anti-inflammatory Activity","authors":"Vijetha Pendyala, V. Suryadevara, Subbarao Jampani, Suhasini Jala","doi":"10.14233/ajomc.2019.ajomc-p217","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p217","url":null,"abstract":"Present study was an attempt to investigate the bioactive components present in the leaves of Guaiacum\u0000officinale using gas chromatography-mass spectroscopy (GC-MS) analysis and study the antiinflammatory\u0000potential of those constituents using molecular docking studies. GC-MS analysis was\u0000done by standard protocol using the equipment JEOL GC MATE II. The identification of components\u0000was based on NIST (National Institute of Standards and Technology) Version-11 library as well as\u0000comparison of their retention indices. The molecular docking studies were done using the commercial\u0000docking software MCULE, 1-click docking. GC-MS analysis of the alcoholic extract showed the\u0000presence of ten compounds at different retention times. The phytoconstituent 8,11,14-eicosatrienoic\u0000acid was present at high concentration with % peak area of 43.3 at a retention time of 19.43 min\u0000followed by 5,7-dihydroxy-8-methoxy flavone (Wogonin) at a retention time of 17.73. All 10 compounds\u0000obtained from GC-MS analysis and diclofenac were used as the ligands in this study, with\u0000cyclooxygenase-2 (COX-2), phospholipase A2 and interleukin receptor as the molecular targets. in silico\u0000Docking studies revealed that the flavanoid Wogonin is having highest binding potential indicated by\u0000least docking score of -8.2, -8 and -6.9 kcal/mol on COX-2, phospholipase A2 and interleukin receptor\u0000respectively.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"42 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85367628","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-10-12DOI: 10.14233/ajomc.2019.ajomc-p221
K. Bijudas, P. Bashpa
Ranitidine hydrochloride is a drug used to treat stomach acid production. It is commonly advised in the treatment of peptic ulcer and gastrophaegal reflux. Ranitidine hydrochloride exists in two different polymorphic forms, namely form I and form II. Various brands of ranitidine hydrochloride tablets manufactured by different pharmaceutical companies in India were collected, finely powdered and recrystallized from ethanol water mixture. The melting points of pure drug samples were determined to assess the polymorphic form present in each sample. All the pure drug samples showed a melting point in the range 135 to 138 °C and prove the existence of polymorph form I. The pure recrystallized drug samples were kept at room temperature for about 60 days in order to study the changes in polymorphic form if any and found fairly stable on prolonged storage. Infrared and UV-visible spectral studies have been carried out by taking Zinetac 150 mg (GlaxoSmithKline Pharmaceuticals Ltd., Mumbai) as the standard in order to prove the chemical constitution of the drug.
{"title":"A comparative Study on Polymorphism of Commercial Ranitidine\u0000Hydrochloride Drug Samples in India","authors":"K. Bijudas, P. Bashpa","doi":"10.14233/ajomc.2019.ajomc-p221","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p221","url":null,"abstract":"Ranitidine hydrochloride is a drug used to treat stomach acid production. It is commonly advised in\u0000the treatment of peptic ulcer and gastrophaegal reflux. Ranitidine hydrochloride exists in two different\u0000polymorphic forms, namely form I and form II. Various brands of ranitidine hydrochloride tablets\u0000manufactured by different pharmaceutical companies in India were collected, finely powdered and\u0000recrystallized from ethanol water mixture. The melting points of pure drug samples were determined to\u0000assess the polymorphic form present in each sample. All the pure drug samples showed a melting point\u0000in the range 135 to 138 °C and prove the existence of polymorph form I. The pure recrystallized drug\u0000samples were kept at room temperature for about 60 days in order to study the changes in polymorphic\u0000form if any and found fairly stable on prolonged storage. Infrared and UV-visible spectral studies have\u0000been carried out by taking Zinetac 150 mg (GlaxoSmithKline Pharmaceuticals Ltd., Mumbai) as the\u0000standard in order to prove the chemical constitution of the drug.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"20 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82767798","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-10-12DOI: 10.14233/ajomc.2019.ajomc-p186
J. Matilda, T. Reji
In an effort to evaluate and design fast, accurate density functional theory (DFT) methods for 5-(4- methoxyphenyl)-3-(1-methylindol-3yl)isoxazole compound was done using Gaussion’ 09 program package using B3LYP method with the 6-31G basis set, which has been successfully applied in order to derive the optimized geometry, bonding features, harmonic vibrational wave numbers, NBO analysis and Mulliken population analysis on atomic charges in the ground state. Optimized geometries of the molecule have been described and collate with the experimental values. The experimental atomic charges demonstrates adequate concurrence with the theoretical prediction from DFT. The theoretical spectra values have been interpreted and compared with the FT-IR spectra. The calculated highest occupied molecular orbital (HOMO) and lowest unoccupied molecular orbital (LUMO) energy gaps also confirm that charge transfer takes place within the molecule.
{"title":"Molecular Structural and Vibrational Spectroscopic Assignments of\u0000n5-(4-Methoxyphenyl)-3-(1-methylindol-3-yl)-isoxazole using DFT Theory Calculations","authors":"J. Matilda, T. Reji","doi":"10.14233/ajomc.2019.ajomc-p186","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p186","url":null,"abstract":"In an effort to evaluate and design fast, accurate density functional theory (DFT) methods for 5-(4-\u0000methoxyphenyl)-3-(1-methylindol-3yl)isoxazole compound was done using Gaussion’ 09 program\u0000package using B3LYP method with the 6-31G basis set, which has been successfully applied in order\u0000to derive the optimized geometry, bonding features, harmonic vibrational wave numbers, NBO analysis\u0000and Mulliken population analysis on atomic charges in the ground state. Optimized geometries of the\u0000molecule have been described and collate with the experimental values. The experimental atomic\u0000charges demonstrates adequate concurrence with the theoretical prediction from DFT. The theoretical\u0000spectra values have been interpreted and compared with the FT-IR spectra. The calculated highest\u0000occupied molecular orbital (HOMO) and lowest unoccupied molecular orbital (LUMO) energy gaps\u0000also confirm that charge transfer takes place within the molecule.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"30 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80385033","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-10-12DOI: 10.14233/ajomc.2019.ajomc-p208
Bhaurao P. Sathe, Harshal S. Oman, N. A. Rehman, P. Dixit, A. Kharat, K. Haval
In the present study, two series of tetrazole containing maleamic (5a-h) and phthaleamic acid (5i-l) derivatives were synthesized and evaluated for their antimicrobial and β-lactamase enzyme inhibition activities. The synthesized compounds were characterized by IR, 1H NMR and 13C NMR spectral techniques. Among the screened compounds, the compound 5c, 5d, 5e, 5f, 5g and 5h have shown good antimicrobial activity. We further performed exploratory β-lactamase enzyme inhibitors studies on β-lactamase.
{"title":"Synthesis, Antimicrobial and β-Lactamase Enzyme Inhibition Activity of Some\u0000New Tetrazole Containing Maleamic and Phthaleamic Acid Derivatives","authors":"Bhaurao P. Sathe, Harshal S. Oman, N. A. Rehman, P. Dixit, A. Kharat, K. Haval","doi":"10.14233/ajomc.2019.ajomc-p208","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p208","url":null,"abstract":"In the present study, two series of tetrazole containing maleamic (5a-h) and phthaleamic acid (5i-l)\u0000derivatives were synthesized and evaluated for their antimicrobial and β-lactamase enzyme inhibition\u0000activities. The synthesized compounds were characterized by IR, 1H NMR and 13C NMR spectral\u0000techniques. Among the screened compounds, the compound 5c, 5d, 5e, 5f, 5g and 5h have shown\u0000good antimicrobial activity. We further performed exploratory β-lactamase enzyme inhibitors studies\u0000on β-lactamase.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":" 4","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91411576","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-10-12DOI: 10.14233/ajomc.2019.ajomc-p193
P. Bansode, I. Somasundaram, Apurva Birajdar, S. Mishra, Dhanashree S. Patil, A. Waghmode, G. Rashinkar
Lonar Crater lake was created by the impact of a massive meteor during the Pleistocene Epoch. Being a hypersaline and hyperalkaline soda lake, rich microbial diversity is reported earlier. Lonar lake water is used by local people and tribals against skin diseases. These observations prompted us to investigate the therapeutic potential of lake water against skin diseases. In this context, we have conducted pilot study to assess the antipsoriatic and antiangiogenic activity of the salt obtained from lake water using THP1 cell line by MTT assay and antiangiogenic activity by in vivo chicken chorioallantoic membrane (CAM) assay, as there is a close relation between psoriasis and angiogenesis. The results revealed that salt possess remarkable antipsoriatic and antiangiogenic activity.
{"title":"Evaluation of Chemical, Antipsoriatic and Antiangiogenic\u0000Properties of Salt from Lonar Crater Lake Water","authors":"P. Bansode, I. Somasundaram, Apurva Birajdar, S. Mishra, Dhanashree S. Patil, A. Waghmode, G. Rashinkar","doi":"10.14233/ajomc.2019.ajomc-p193","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p193","url":null,"abstract":"Lonar Crater lake was created by the impact of a massive meteor during the Pleistocene Epoch. Being\u0000a hypersaline and hyperalkaline soda lake, rich microbial diversity is reported earlier. Lonar lake\u0000water is used by local people and tribals against skin diseases. These observations prompted us to\u0000investigate the therapeutic potential of lake water against skin diseases. In this context, we have\u0000conducted pilot study to assess the antipsoriatic and antiangiogenic activity of the salt obtained from\u0000lake water using THP1 cell line by MTT assay and antiangiogenic activity by in vivo chicken\u0000chorioallantoic membrane (CAM) assay, as there is a close relation between psoriasis and angiogenesis.\u0000The results revealed that salt possess remarkable antipsoriatic and antiangiogenic activity.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"40 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79793492","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-10-12DOI: 10.14233/ajomc.2019.ajomc-p213
S. Devkate, A. Burungale, A. Pise, S. Jadhav
The regioselective epoxide ring opening at less substituted carbon atom of epoxide were reported by nucleophiles like heterocyclic amines which gives well known 1,2-difunctionalized amino alcohols. These are present in many synthetic as well as natural products. The ring opening of epoxide is achieved by cleavage with amines in presence of copper(0) as a catalyst. It is observed that the lithium napthalenide reduction of copper(I) produces a highly reactive form of copper(0) that acts as a catalyst for ring opening of epoxides with an amine.
{"title":"Active Copper Catalyzed Regioselective Ring Opening of Epoxides by Heterocyclic\u0000Amines: An Efficient Protocol for Synthesis of β-Amino Alcohols","authors":"S. Devkate, A. Burungale, A. Pise, S. Jadhav","doi":"10.14233/ajomc.2019.ajomc-p213","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p213","url":null,"abstract":"The regioselective epoxide ring opening at less substituted carbon atom of epoxide were reported by\u0000nucleophiles like heterocyclic amines which gives well known 1,2-difunctionalized amino alcohols.\u0000These are present in many synthetic as well as natural products. The ring opening of epoxide is achieved\u0000by cleavage with amines in presence of copper(0) as a catalyst. It is observed that the lithium\u0000napthalenide reduction of copper(I) produces a highly reactive form of copper(0) that acts as a catalyst\u0000for ring opening of epoxides with an amine.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"131 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77680739","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-05-01DOI: 10.14233/AJOMC.2019.AJOMC-P166
K. Kumar, R. V. Nadh, M. Kishore, G. Prasad
A simple, selective, accurate and low-cost spectrophotometric method has been described for determination of satranidazole in bulk and pharmaceutical formulations. The developed method involves the formation of chloroform extractable colored ion-association complex of satranidazole with Tropaeolin OOO (TPooo). The extracted colored complex showed absorbance maximum at wavelength 484 nm and obeying Beer′s law in the concentration 4-20 μg mL-1 with the correlation coeffiecent of 0.9998. The results of statistical analysis of the proposed method reveals high accuracy and good precession. Thus, the proposed method can be used commercially for the determination of satranidazole in bulk and pharmaceutical formulations.
{"title":"Determination of Satranidazole through Ion-Associative Complex Reaction","authors":"K. Kumar, R. V. Nadh, M. Kishore, G. Prasad","doi":"10.14233/AJOMC.2019.AJOMC-P166","DOIUrl":"https://doi.org/10.14233/AJOMC.2019.AJOMC-P166","url":null,"abstract":"A simple, selective, accurate and low-cost spectrophotometric method has been described for determination of satranidazole in bulk and pharmaceutical formulations. The developed method involves the formation of chloroform extractable colored ion-association complex of satranidazole with Tropaeolin OOO (TPooo). The extracted colored complex showed absorbance maximum at wavelength 484 nm and obeying Beer′s law in the concentration 4-20 μg mL-1 with the correlation coeffiecent of 0.9998. The results of statistical analysis of the proposed method reveals high accuracy and good precession. Thus, the proposed method can be used commercially for the determination of satranidazole in bulk and pharmaceutical formulations.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"33 22","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91435989","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-03-30DOI: 10.14233/AJOMC.2019.AJOMC-P171
Jaman A. Angulwar, G. Khansole, V. Bhosale
2-Amino-5-phenyl-1,3,4-thiadiazole on reaction with ethyl-2-cyano-3,3-bis(methylthio)acrylate in the presence of N,N′-dimethyl formamide and catalytic amount of anhydrous potassium carbonate afforded 7-(methylthio)-5-oxo-2-phenyl-5H-[1,3,4]thiadiazolo[3,2-b]pyrimidine- 6-carbonitrile under similar experimental condition, compounds 7-(methylthio)-5-oxo-2-phenyl-5H-[1,3,4]thiadiazolo[3,2-b]pyrimidine-6-carbonitrile on treatment independently with aryl amines/ heteryl amines/phenols containing active methylene group yielded correspon-ding 7-substituted derivatives. All these newly synthesized compounds were screened for antimicrobial activity.
{"title":"Novel Synthesis and Antimicrobial Activity of 7-Substituted Derivatives of 7-(methylthio)-5-oxo-2-phenyl-5H-[1,3,4]thiadiazolo[3,2-b]- pyrimidine-6-carbonitrile","authors":"Jaman A. Angulwar, G. Khansole, V. Bhosale","doi":"10.14233/AJOMC.2019.AJOMC-P171","DOIUrl":"https://doi.org/10.14233/AJOMC.2019.AJOMC-P171","url":null,"abstract":"2-Amino-5-phenyl-1,3,4-thiadiazole on reaction with ethyl-2-cyano-3,3-bis(methylthio)acrylate in the presence of N,N′-dimethyl formamide and catalytic amount of anhydrous potassium carbonate afforded 7-(methylthio)-5-oxo-2-phenyl-5H-[1,3,4]thiadiazolo[3,2-b]pyrimidine- 6-carbonitrile under similar experimental condition, compounds 7-(methylthio)-5-oxo-2-phenyl-5H-[1,3,4]thiadiazolo[3,2-b]pyrimidine-6-carbonitrile on treatment independently with aryl amines/ heteryl amines/phenols containing active methylene group yielded correspon-ding 7-substituted derivatives. All these newly synthesized compounds were screened for antimicrobial activity.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89803201","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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