Synthesis and evaluation of anti-inflammatory and analgesic activity of 3-[(5-substituted-1,3,4-oxadiazol-2-yl-thio)acetyl]-2H-chromen-2-ones |
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| Authors: | Nista Ingale Veeresh Maddi Mahesh Palkar Pradeepkumar Ronad Shivalingrao Mamledesai A H M Vishwanathswamy Darbhamulla Satyanarayana |
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| Institution: | (1) Department of Pharmaceutical Chemistry, KLES’ College of Pharmacy, Vidyanagar, Hubli, 580031, Karnataka, India;(2) Department of Pharmacology, KLES’ College of Pharmacy, Vidyanagar, Hubli, 580031, Karnataka, India;(3) Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, Paneer, Deralakatte, Mangalore, Karnataka, India; |
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| Abstract: | A novel series of 3-(5-substituted-1,3,4-oxadiazol-2-yl-thio)acetyl]-2H-chromen-2-one (7a–i) were synthesized by the condensation between the appropriately substituted 5-substituted-1,3,4-oxadiazolyl-2-thione (4a–i) derived from various existing NSAIDs and 3-(2-bromoacetyl)-2H-chromen-2-one (6) under reflux in the presence of sodium ethoxide. Structure of the synthesized compounds was established on the basis of
physicochemical, elemental analysis, and spectral data. The title compounds were screened for in vivo acute anti-inflammatory
and analgesic activities at a dose of 200 mg/kg bw. Among the series, four compounds 7c, 7e, 7f, and 7h were found to possess a significant anti-inflammatory and analgesic activity profile. In addition, these compounds were also
found to possess a less degree of ulcerogenic potential as compared to standard NSAIDs. |
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