Author
Shankar G. Alegaon
Bio: Shankar G. Alegaon is an academic researcher. The author has contributed to research in topics: Pyrazole & Docking (molecular). The author has an hindex of 11, co-authored 22 publications receiving 405 citations.
Topics: Pyrazole, Docking (molecular), DNA gyrase, Chemistry, 4-Aminoquinoline
Papers
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TL;DR: The present study suggests that compounds 6b, 6c, 6d, 6e and 6f may serve as promising lead scaffolds for further generation of new anti-TB agents.
118 citations
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TL;DR: The cyclooxygenase (COX) enzyme inhibitor activity of selected compounds, which are the excellent anti-inflammatory activities in carrageenan-induced paw edema model, was investigated in vitro COX inhibition assay and molecular docking study further helped in supporting the observed activity.
66 citations
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TL;DR: The synthesis and antimicrobial activity of 2,4-thiazolidinedione derivatives 5a–g and 6a-g showed high or moderate biological activity against tested microorganisms.
59 citations
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TL;DR: The result of present study suggests that pyrazole-thiadiazole hybrid could be an interesting approach for the design of new selective COX-2 inhibitory agents.
38 citations
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TL;DR: The preliminary results revealed that the compound 3d exhibits promising antibacterial and antifungal activity and compound 3j inhibited proliferation of HeLa, HT29, A549 and MCF-7 cell lines with IC50 values of 33, 35, 30 and 36 μM, respectively.
Abstract: The present work describes the synthesis, antimicrobial and cytotoxic activity of 2,4-thiazolidinedione-5-acetic acid amides 3a–n. The structures of the compounds were confirmed by IR, 1H, 13C NMR and elemental analysis. All compounds were tested for antimicrobial activity by twofold serial dilution technique. The preliminary results revealed that the compound 3d exhibits promising antibacterial and antifungal activity. The cytotoxic (MTT) activity of 2,4-thiazolidinedione-5-acetic acid amides were tested in four tumour cell lines. We found that compound 3j inhibited proliferation of HeLa, HT29, A549 and MCF-7 cell lines with IC50 values of 33, 35, 30 and 36 μM, respectively.
34 citations
Cited by
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TL;DR: The synthetic isoquinoline alkaloid virstatin, for example, inhibits the transcriptional regulator ToxT in Vibrio cholerae, preventing expression of cholera toxin and fimbriae and conferring in vivo protection against intestinal colonisation.
564 citations
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TL;DR: The different synthesis methods and the pharmacological properties of pyrazole derivatives developed by many scientists around the globe are highlighted.
Abstract: Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antipsychotic CDPPB, the anti-obesity drug rimonabant, difenamizole, an analgesic, betazole, a H2-receptor agonist and the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. Owing to this diversity in the biological field, this nucleus has attracted the attention of many researchers to study its skeleton chemically and biologically. This review highlights the different synthesis methods and the pharmacological properties of pyrazole derivatives. Studies on the synthesis and biological activity of pyrazole derivatives developed by many scientists around the globe are reported.
520 citations
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366 citations
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TL;DR: The structures of 1H-pyrazoles with their corresponding biological activities for 21st (in 2000-2014 years) century are reported.
312 citations
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TL;DR: Owing to the development of novel and new pyrazole based therapeutic agents at a faster pace, there is a need to couple the latest information with previously available information to understand status of this moiety in medicinal chemistry research.
286 citations