Journal of Chemical and Pharmaceutical Research (ISSN : 0975-7384)

header
Reach Us reach to JOCPR whatsapp-JOCPR +44 1625708989
All submissions of the EM system will be redirected to Online Manuscript Submission System. Authors are requested to submit articles directly to Online Manuscript Submission System of respective journal.

Original Articles: 2016 Vol: 8 Issue: 2

Synthesis and preliminary evaluation of potential highly selective COX-2 inhibitors of some nonsteroidal anti-inflammatory derivatives

Abstract

This work include design and synthesis of novel nonsteroidal anti-inflammatory(NSAI) derivatives, with potential selectivity cyclooxygenase 2(COX- 2) inhibitors from well-known NSAIDs ,to increase or at least maintain antiinflammatory activity, and decrease adverse effects resulting from COX-1 inhibition .Six compounds were synthesized ,(compound 2and 3) from aspirin with 4-(4-Fluorophenyl)isoxazol-5-amine and 6-chloro,2- aminobenzothiazole, (compound 6and 7) from diflunisal with 4-(4-Fluorophenyl)isoxazol-5-amine and 3-methyl-4- [3-(trifluoromethyl) phenyl]-5-isoxazolamine, (compound 9 and 10) from Ketoprofen with 2-Amino-5- (trifluoromethyl)1,3,4-thiadiazole and 2-Amino-5-ethyl 1,3,4-thiadiazole.Analysis by IR and 1H-NMR were performed and consistent with proposed synthesized structures. The preliminary pharmacological evaluation as anti-inflammatory activity test and ulcerogenic index screening were performed. From results of both test, we see most derivative showed good anti-inflammatory activity with range from46.5%(compound 2) to 36.2% (compound9) compared to 41% (standard) as %paw edema inhibition, but compound 2 and compound 6 showed ulcer index analogous to celecoxib a selective COX-2 inhibitors as a safe standard of gastric irritation.