One pot synthesis of thiazolo2,3-bdihydropyrimidinone possessing pyrazole moiety and evaluation of their anti-inflammatory and antimicrobial activities

Viveka, S. and Dinesha and Nagaraja, G. K. and Shama, Prasanna and Basavarajaswamy, Guru and Rao, K. Poornachandra and Sreenivasa, M. Y. (2018) One pot synthesis of thiazolo2,3-bdihydropyrimidinone possessing pyrazole moiety and evaluation of their anti-inflammatory and antimicrobial activities. Medicinal Chemistry Research, 27 (1). pp. 171-185. ISSN 1554-8120

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Abstract

A series of pyrazole integrated thiazolo2,3-bdihydropyrimidinone 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 thiazolo2,3-bdihydropyrimidinone 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:	C Chemical Science > Chemistry
Divisions:	Department of > Chemistry
Depositing User:	LA manjunath user
Date Deposited:	16 Oct 2019 10:12
Last Modified:	11 Dec 2019 09:48
URI:	http://eprints.uni-mysore.ac.in/id/eprint/9218

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