One pot synthesis of thiazolo[2,3-b]dihydropyrimidinone possessing pyrazole moiety and evaluation of their antiinflammatory and antimicrobial activities

Viveka, S. and Dinesha and Nagaraja, G. K. and Shama, P. and Basavarajaswamy, G. and Rao, K. P. and Sreenivasa, M. Y. (2018) One pot synthesis of thiazolo[2,3-b]dihydropyrimidinone possessing pyrazole moiety and evaluation of their antiinflammatory and antimicrobial activities. Medicinal Chemistry Research, 27. pp. 171-185. ISSN 1554-8120

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Official URL: https://doi.org/10.1007/s00044-017-2058-8

Abstract

A series of pyrazole integrated thiazolo[2,3-b]dihydropyrimidinone derivatives were synthesized as dual anti-inflammatory and antimicrobial agents. Among the compounds studied, 3-fluoro-4-methylphenyl analogues (3a, 3e, and 3i) are considered to be promising leads for novel anti-inflammatory agents compared with the standard drug. The superior antimicrobial property of the compounds 3a, 3b, and 3d indicates that 3-(3,4-dichlorophenyl)-1-phenyl-1H-pyrazole substitution is a favourable site for high activity. Molecular docking studies were carried out in order to predict the hypothetical binding mode of these compounds to the COX-2 isoenzyme. The results of the present study suggest that 1,3-diaryl pyrazole substitution on thiazolo[2,3-b]dihydropyrimidinone derivatives might potentially constitute a novel class of anti-inflammatory agents with antimicrobial property and could be an interesting approach for the design of new selective COX-2 inhibitory agents.

Item Type: Article
Subjects: B Life Science > Microbiology
Divisions: Department of > Microbiology
Depositing User: Arshiya Kousar
Date Deposited: 09 Oct 2019 11:47
Last Modified: 09 Oct 2019 11:48
URI: http://eprints.uni-mysore.ac.in/id/eprint/8802

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