Pub Date : 2021-03-16DOI: 10.56042/ijcb.v60i3.41338
{"title":"Synthesis and biological evaluation of novel 3-aryl-4-methoxy N-alkyl maleimides","authors":"","doi":"10.56042/ijcb.v60i3.41338","DOIUrl":"https://doi.org/10.56042/ijcb.v60i3.41338","url":null,"abstract":"","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2021-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74807996","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-03-16DOI: 10.56042/ijcb.v60i3.28816
{"title":"New macromolecular structures based on benzene core, synthesis and characterization","authors":"","doi":"10.56042/ijcb.v60i3.28816","DOIUrl":"https://doi.org/10.56042/ijcb.v60i3.28816","url":null,"abstract":"","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2021-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79059434","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-03-16DOI: 10.56042/ijcb.v60i3.31796
{"title":"Synthesis, in vitro biological evaluation and molecular docking study of coumarin-1,4-dihydropyridine derivatives as potent anti-inflammatory agents","authors":"","doi":"10.56042/ijcb.v60i3.31796","DOIUrl":"https://doi.org/10.56042/ijcb.v60i3.31796","url":null,"abstract":"","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2021-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83208670","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-03-16DOI: 10.56042/ijcb.v60i3.32259
{"title":"Synthesis and anticonvulsant activity of some 1,4-dihydropyridine derivatives","authors":"","doi":"10.56042/ijcb.v60i3.32259","DOIUrl":"https://doi.org/10.56042/ijcb.v60i3.32259","url":null,"abstract":"","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2021-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86633856","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-03-16DOI: 10.56042/ijcb.v60i3.38659
{"title":"Synthesis, in silico pharmacokinetic analysis and anticancer activity evaluation of benzothiazole-triazole hybrids","authors":"","doi":"10.56042/ijcb.v60i3.38659","DOIUrl":"https://doi.org/10.56042/ijcb.v60i3.38659","url":null,"abstract":"","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2021-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85675676","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-02-15DOI: 10.56042/ijcb.v60i2.29657
I. Mamedov, Y. Mamedova
The aromatic ketones are effective compounds in organic synthesis and have important significance for synthesis of different practical compounds, which have physiological activity. Due to the their different functionality these compounds confer biological activities, such as antimicrobial, antibacterial, antifungal, anticancer, antiviral, anti-inflammatory, antihyperglycemic. Taking into account of their pharmaceutical actuality the 1,2,3,4,5-pentasubstituted cyclohexanol and its forming chalcone against S. aureus, E. coli, KES (Klebsiella, Enterobacter, Serratia) and A. niger were investigated.
{"title":"Biological activity of novel pentasubstituted cyclohexanol against some microorganisms","authors":"I. Mamedov, Y. Mamedova","doi":"10.56042/ijcb.v60i2.29657","DOIUrl":"https://doi.org/10.56042/ijcb.v60i2.29657","url":null,"abstract":"The aromatic ketones are effective compounds in organic synthesis and have important significance for synthesis of different practical compounds, which have physiological activity. Due to the their different functionality these compounds confer biological activities, such as antimicrobial, antibacterial, antifungal, anticancer, antiviral, anti-inflammatory, antihyperglycemic. Taking into account of their pharmaceutical actuality the 1,2,3,4,5-pentasubstituted cyclohexanol and its forming chalcone against S. aureus, E. coli, KES (Klebsiella, Enterobacter, Serratia) and A. niger were investigated.","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2021-02-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77550494","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-02-15DOI: 10.56042/ijcb.v60i2.30155
{"title":"In vitro anticancer activity of thiazole based β-amino carbonyl derivatives against HCT116 and H1299 colon cancer cell lines; study of pharmacokinetics, physicochemical, medicinal properties and molecular docking analysis","authors":"","doi":"10.56042/ijcb.v60i2.30155","DOIUrl":"https://doi.org/10.56042/ijcb.v60i2.30155","url":null,"abstract":"","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2021-02-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82935982","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-02-15DOI: 10.56042/ijcb.v60i2.32682
Viveka Fonsecaa, S. Chandavarkar, Renuka Dabholkara, Prachita Gauns Dessaia, Mangirish Deshpandec, Shivalingrao N Mamle Desaia
The present investigation deals with molecular docking, synthesis, characterization, and evaluation of in vitro tyrosine kinase inhibitor activity of a series of 4-[2-(substituted phenyl) hydrazono]-3-(1-hydroxyethyl)-1-phenyl/methyl-3,4-dihydroquinolin-2(1 H )-one derivatives {III-a(1-12)/III-b(1-12)}. Molecular docking studies of the title compounds were carried out using Molegro Virtual Docker (MVD-2013, 6.0) software. The MolDock scores of the derivatives ranged from ( − 66.508) to ( − 101.274); whereas the MolDock score of standard 4-anilinoquinazoline ligand was found to be ( − 105.219). Most of the synthesized qunolin-2-one derivatives showed better affinity towards EGFRK protein as compared to standard drug imatinib ( − 104.253). All the synthesized compounds were satisfactorily characterized by physical and spectral analysis (UV, IR, 1 H NMR and 13 C NMR and mass spectral data). Twelve derivatives were tested for their in vitro tyrosine kinase inhibitor activity using MDA-MB cell line. Compound 4-[2-(4-bromophenyl)hydrazono]-3-(1-hydroxyethyl)-1-methyl- 3,4-dihydroquinolin-2(1 H )-one (III-b4) was found to be the most cytotoxic compound as compared to other synthesized derivatives, with IC 50 value of 0.0515 μ M against MDA- MB cell line.
{"title":"Design, synthesis of 4-[2-(substituted phenyl) hydrazono]-3-(1-hydroxyethyl)-1-phenyl/methyl-3,4-dihydroquinolin-2(1H)-one derivatives and evaluation of their in vitro tyrosine kinase inhibitor activity","authors":"Viveka Fonsecaa, S. Chandavarkar, Renuka Dabholkara, Prachita Gauns Dessaia, Mangirish Deshpandec, Shivalingrao N Mamle Desaia","doi":"10.56042/ijcb.v60i2.32682","DOIUrl":"https://doi.org/10.56042/ijcb.v60i2.32682","url":null,"abstract":"The present investigation deals with molecular docking, synthesis, characterization, and evaluation of in vitro tyrosine kinase inhibitor activity of a series of 4-[2-(substituted phenyl) hydrazono]-3-(1-hydroxyethyl)-1-phenyl/methyl-3,4-dihydroquinolin-2(1 H )-one derivatives {III-a(1-12)/III-b(1-12)}. Molecular docking studies of the title compounds were carried out using Molegro Virtual Docker (MVD-2013, 6.0) software. The MolDock scores of the derivatives ranged from ( − 66.508) to ( − 101.274); whereas the MolDock score of standard 4-anilinoquinazoline ligand was found to be ( − 105.219). Most of the synthesized qunolin-2-one derivatives showed better affinity towards EGFRK protein as compared to standard drug imatinib ( − 104.253). All the synthesized compounds were satisfactorily characterized by physical and spectral analysis (UV, IR, 1 H NMR and 13 C NMR and mass spectral data). Twelve derivatives were tested for their in vitro tyrosine kinase inhibitor activity using MDA-MB cell line. Compound 4-[2-(4-bromophenyl)hydrazono]-3-(1-hydroxyethyl)-1-methyl- 3,4-dihydroquinolin-2(1 H )-one (III-b4) was found to be the most cytotoxic compound as compared to other synthesized derivatives, with IC 50 value of 0.0515 μ M against MDA- MB cell line.","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2021-02-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89941995","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-02-15DOI: 10.56042/ijcb.v60i2.30182
{"title":"Synthesis of a new heterocyclic dye compound as an indicator in acid and base reactions","authors":"","doi":"10.56042/ijcb.v60i2.30182","DOIUrl":"https://doi.org/10.56042/ijcb.v60i2.30182","url":null,"abstract":"","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2021-02-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80921432","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-02-15DOI: 10.56042/ijcb.v60i2.30279
Attreyee Mukherjeea, K. K. Mahalanabis
Acylation of methyl 3-aminocrotonate 1a in benzene with a variety of aliphatic and aromatic acid chlorides including α , β -unsaturated acid chloride in the presence of an added organic base, (either pyridine or triethylamine) is reported. The preferred N, C-site selectivity in these reactions has been compared with the terminal selectivity of the products obtained previously on acylation of methyl 3-aminocrotononitrile 1b . A strong preference either for N- or C- selectivity in N, C-acylation has been observed for both 1a and 1b based on the choice of acid chlorides and added organic base. Interestingly, irrespective of the enamine 1a or 1b , acylation with α , β -unsaturated acid chlorides in the presence of triethylamine afforded 3,4-dihydropyridin-(2 H )-one via [3.3] sigmatropic rearrangement of the corresponding intermediary N(E)-enamide. Accrued results show methyl 3-aminocrotonate to be a better precursor for preparation of enamides (N-acylated products) whereas 3-aminocrotononitrile is found to be a preferred choice for preparation of enaminones (C-acylated products). An attempt is made to offer a preliminary theoretical interpretation for observed site selectivity.
{"title":"Systematic study on acylation of methyl 3-aminocrotonate with acid chlorides of aliphatic, aromatic and α, β-unsaturated acids: A comparative evaluation of the preference for regio- and stereoselectivity vis-à-vis 3-aminocrotononitrile","authors":"Attreyee Mukherjeea, K. K. Mahalanabis","doi":"10.56042/ijcb.v60i2.30279","DOIUrl":"https://doi.org/10.56042/ijcb.v60i2.30279","url":null,"abstract":"Acylation of methyl 3-aminocrotonate 1a in benzene with a variety of aliphatic and aromatic acid chlorides including α , β -unsaturated acid chloride in the presence of an added organic base, (either pyridine or triethylamine) is reported. The preferred N, C-site selectivity in these reactions has been compared with the terminal selectivity of the products obtained previously on acylation of methyl 3-aminocrotononitrile 1b . A strong preference either for N- or C- selectivity in N, C-acylation has been observed for both 1a and 1b based on the choice of acid chlorides and added organic base. Interestingly, irrespective of the enamine 1a or 1b , acylation with α , β -unsaturated acid chlorides in the presence of triethylamine afforded 3,4-dihydropyridin-(2 H )-one via [3.3] sigmatropic rearrangement of the corresponding intermediary N(E)-enamide. Accrued results show methyl 3-aminocrotonate to be a better precursor for preparation of enamides (N-acylated products) whereas 3-aminocrotononitrile is found to be a preferred choice for preparation of enaminones (C-acylated products). An attempt is made to offer a preliminary theoretical interpretation for observed site selectivity.","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2021-02-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84986864","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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