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N-(1,3-Diaryl-3-oxopropyl)amides as a new template for xanthine oxidase inhibitors
Authors:Nepali Kunal  Agarwal Amit  Sapra Sameer  Mittal Vineet  Kumar Raj  Banerjee Uttam C  Gupta Manish K  Satti Naresh K  Suri Om P  Dhar Kanaya L
Institution:Laboratory for Drug Design and Synthesis, Department of Pharmaceutical Chemistry, Indo-Soviet Friendship College of Pharmacy, Moga 142 001, Punjab, India.
Abstract:A series of forty two N-(1,3-diaryl-3-oxopropyl)amides were synthesized via an efficient, modified Dakin-West reaction and were evaluated for in vitro xanthine oxidase inhibitory activity for the first time. Structure-activity relationship analyses have been presented. Selected active xanthine oxidase inhibitors (3r, 3s, and 3zh) were assessed in vivo to study their anti-hyperuricemic effect in potassium oxonate induced hyperuricemic mice model. Compound 3s emerged as the most potent xanthine oxidase inhibitor (IC(50)=2.45 μM) as well as the most potent anti-hyperuricemic agent. The basis of significant inhibition of xanthine oxidase by 3s was rationalized by its molecular docking into catalytic site of xanthine oxidase.
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