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

Title: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

Volume: 11 Issue: 8

Author(s): Kaliappan Ilango, Parthiban Valentina, Gajendra Kumar, Dushyant Dixit, Shrikant Nilewar and Muthu K. Kathiravan

Affiliation:

Keywords: 1, 3, 4-oxadizole, NSAID, anti-inflammatory, analgesic, QSAR.

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

Cite this article as:

Ilango Kaliappan, Valentina Parthiban, Kumar Gajendra, Dixit Dushyant, Nilewar Shrikant and Kathiravan K. Muthu, 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, Medicinal Chemistry 2015; 11 (8) . https://dx.doi.org/10.2174/1573406411666150519112037