Nepali, Kunal and Agarwal, Amit and Sapra, Sameer and Mittal, Vineet and Kumar, Raj and Banerjee, Uttam C. and Gupta, Manish K. and Satti, Naresh K. and Suri, Om P. and Dhar, Kanaya L. (2011) N-(1,3-Diaryl-3-oxopropyl)amides as a new template for xanthine oxidase inhibitors. Bioorganic & Medicinal Chemistry, 19 (18). pp. 5569-5576. ISSN 09680896

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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 (IC50 = 2.45 lM) 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.

Item Type: Article
Subjects: Chemical Sciences
Depositing User: Mr. Amit Nargotra
Date Deposited: 02 Jan 2012 10:54
Last Modified: 02 Jan 2012 10:54

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