N-(1,3-Diaryl-3-oxopropyl)amides as a new template for xanthine oxidase inhibitors |
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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 |
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Institution: | Laboratory for Drug Design and Synthesis, Department of Pharmaceutical Chemistry, Indo-Soviet Friendship College of Pharmacy, Moga 142 001, Punjab, India. |
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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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