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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

[ Vol. 11 , Issue. 8 ]

Author(s):

Kaliappan Ilango, Parthiban Valentina, Gajendra Kumar, Dushyant Dixit, Shrikant Nilewar and Muthu K. Kathiravan   Pages 753 - 763 ( 11 )

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

Keywords:

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

Affiliation:

Department of Pharmaceutical Chemistry, SRM College of Pharmacy, SRM University, Kattankulathur - 603 203, Kancheepuram (Dt), Tamil Nadu, India.

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