Design, synthesis and QSAR studies on a series of 2, 5-disubstituted- 1,3,4-oxadiazole derivatives of diclofenac and naproxen for analgesic and anti-inflammatory activity.

Abstract

A series of twenty molecules belonging to 2,5-disubstituted-1,3,4-oxadiazole derivatives of Diclofenac and Naproxen were designed, synthesized and their structures were confirmed by spectroscopy. The target compounds were evaluated for anti-inflammatory and analgesic activity. The result indicates that the compounds 12, 4, 6, 7 and 15 were found to have good analgesic and anti-inflammatory activities, while the compounds 12 and 14 were found to have good analgesic and the compound 22 were found to have good anti-inflammatory activities. HQSAR and Topomer QSAR studies were performed to get insights in the structures contributing for biological activity. The compounds bearing mono-substitution such as Cl, OCH3 and NO2 in the phenyl ring were found to have maximum analgesic and anti-inflammatory activities.