1338705-53-5Relevant academic research and scientific papers
N-(1,3-Diaryl-3-oxopropyl)amides as a new template for xanthine oxidase inhibitors
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.
experimental part, p. 5569 - 5576 (2011/10/19)
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.
