Research paperDesign, synthesis and biological evaluation of N-(4-alkoxy-3-cyanophenyl)isonicotinamide/nicotinamide derivatives as novel xanthine oxidase inhibitors

Add time:09/02/2019    Source:sciencedirect.com

A series of N-(4-alkoxy-3-cyanophenyl)isonicotinamide/nicotinamide derivatives was designed, synthesized and evaluated for inhibitory potency in vitro against xanthine oxidase. The isonicotinamide series was considerably more effective than the nicotinamide series. SARs analysis revealed that the isonicotinoyl moiety played a significant role on the inhibition and that a benzyl ether tail (e.g., ortho-cyanobenzoxy) linked to the benzonitrile moiety benefits the inhibitory potency. Among these compounds, 10q (IC50 = 0.3 μM) was identified to be the most potent in this work and was observed to be 28.3-fold more potent than allopurinol but 20-fold less potent than topiroxostat. The Lineweaver-Burk plot showed that 10q acted as a mixed-type inhibitor on xanthine oxidase. Molecular modeling provided a reasonable explanation for the SARs observed in this study.

We also recommend Trading Suppliers and Manufacturers of 4-cyanophenyl acetate (cas 13031-41-9). Pls Click Website Link as below: cas 13031-41-9 suppliers

Prev:Green synthesis of fluorapatite from waste animal bones and the photo-catalytic degradation activity of a new ZnO/green biocatalyst nano-composite for removal of chlorophenols
Next:Synthesis and photophysical properties of N,N′-bis(4-cyanophenyl)-3,4,9,10-perylenebis(dicarboximide) and N,N′-bis(4-cyanophenyl)-1,4,5,8-naphthalenediimide)