N-(1,3-Diaryl-3-oxopropyl)amides as a new template for xanthine oxidase inhibitors

Add time:08/01/2019    Source:sciencedirect.com

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 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.

We also recommend Trading Suppliers and Manufacturers of 3-(3-amino-3-oxopropyl)-2-[[1-methyl-2-(p-tolyl)-1H-indol-3-yl]azo]benzothiazolium chloride (cas 12221-63-5). Pls Click Website Link as below: cas 12221-63-5 suppliers

Prev:Supramolecular architecture, spectroscopic properties and stability of C.I. Basic Violet 10 (Rhodamine B) at high concentration
Next:Modified C.I. Pigment Red 170 with a core-shell structure: Preparation, characterization and computational study)