Design, synthesis, antinociceptive, and anti-inflammatory properties of thiazolopyrimidine derivatives

Abstract

Ten 2-(substituted benzylidene)-7-(4-chlorophenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a]pyrimidin-3(7H)-one derivatives were synthesized and evaluated. A series of heterocyclic, 2-(substituted benzylidene)-7-(4-chlorophenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a]pyrimidin-3(7H)-one were synthesized by reaction of 7-(4-chloro phenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a]pyrimidin-3(7H)-one with appropriately substituted aldehydes in the presence of anhydrous sodium acetate and glacial acetic acid. The antinociceptive activity was evaluated by tail-flick technique, anti-inflammatory activity was evaluated by carrageenan-induced paw edema test and their ulcerogenicity index was determined. The para-substituted methyl, hydroxy, fluoro, chloro, bromo, and nitro derivatives showed significant antinociceptive and anti-inflammatory activities. The detailed synthesis, spectroscopic data, and pharmacological screening of the synthesized compounds were reported.

Keywords:

• thiazolopyrimidine
• antinociceptive activity
• anti-inflammatory activity

Acknowledgments

The authors gratefully acknowledge the chemistry department at PES's Rajaram and Tarabai Bandekar College of Pharmacy for all facilities provided in terms the use of the available chemicals and equipments. Also, we would like to thank the Central Instrumentation Facility, IIT Chennai, India, for the spectral analysis of the compounds used in this study.