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. 2010 Feb;45(2):800-4.
doi: 10.1016/j.ejmech.2009.11.003. Epub 2009 Nov 6.

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

Franco Chimenti  1 , Simone Carradori, Daniela Secci, Adriana Bolasco, Bruna Bizzarri, Paola Chimenti, Arianna Granese, Matilde Yáñez, Francisco Orallo
Affiliations

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

Franco Chimenti et al. Eur J Med Chem. 2010 Feb.

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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