Synthesis and inhibitory activity against human monoamine oxidase of N1-thiocarbamoyl-3,5-di(hetero)aryl-4,5-dihydro-(1H)-pyrazole derivatives

European Journal of Medicinal Chemistry
Franco ChimentiFrancisco Orallo

Abstract

A series of N1-thiocarbamoyl-3,5-di(hetero)aryl-4,5-dihydro-(1H)-pyrazole derivatives has been synthesized and assayed for their ability to inhibit the activity of the A and B isoforms of human monoamine oxidase (hMAO). Some of these compounds were endowed with a selective inhibitory activity against hMAO-B in the micromolar range. The most active of the series is the compound 13, N1-thiocarbamoyl-3-(fur-2'-yl)-5-(4'-fluoro-phenyl)-4,5-dihydro-(1H)-pyrazole, with IC(50) 2.75+/-0.81muM value and selectivity ratio of 25, which is the best candidate for further investigations.

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Citations

Jan 31, 2013·Journal of Neural Transmission·Umut Salgin-GökşenNesrin Gökhan-Kelekçi
Oct 9, 2013·European Journal of Medicinal Chemistry·B Vishnu NayakVenkatesan Jayaprakash
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