1. One pot synthesis of thiazolo[2,3-b]dihydropyrimidinone possessing pyrazole moiety and evaluation of their anti-inflammatory and antimicrobial activities
- Author
-
Marikunte Yanjarappa Sreenivasa, Dinesha, Guru Basavarajaswamy, Prasanna Shama, Gundibasappa Karikannar Nagaraja, K. Poornachandra Rao, and Shivapura Viveka
- Subjects
010405 organic chemistry ,Chemistry ,medicine.drug_class ,Stereochemistry ,Organic Chemistry ,One-pot synthesis ,Pharmacology toxicology ,Pyrazole ,010402 general chemistry ,Antimicrobial ,01 natural sciences ,Combinatorial chemistry ,Anti-inflammatory ,0104 chemical sciences ,chemistry.chemical_compound ,medicine ,Moiety ,High activity ,General Pharmacology, Toxicology and Pharmaceutics - 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.
- Published
- 2017
- Full Text
- View/download PDF