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 +/- 0.81 mu M value and selectivity ratio of 25, which is the best candidate for further investigations. (C) 2009 Elsevier Masson SAS. All rights reserved.
Synthesis and inhibitory activity against human monoamine oxidase of N1-thiocarbamoyl-3,5-di(hetero)aryl-4,5-dihydro-(1H)-pyrazole derivatives / Chimenti, Franco; Carradori, Simone; Secci, Daniela; Bolasco, Adriana; Bizzarri, Bruna; Chimenti, Paola; Arianna, Granese; Matilde, Yanez; Francisco, Orallo. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - STAMPA. - 45:2(2010), pp. 800-804. [10.1016/j.ejmech.2009.11.003]
Synthesis and inhibitory activity against human monoamine oxidase of N1-thiocarbamoyl-3,5-di(hetero)aryl-4,5-dihydro-(1H)-pyrazole derivatives
CHIMENTI, Franco;CARRADORI, Simone;SECCI, DANIELA;BOLASCO, Adriana;BIZZARRI, Bruna;CHIMENTI, Paola;Arianna Granese;
2010
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 +/- 0.81 mu M value and selectivity ratio of 25, which is the best candidate for further investigations. (C) 2009 Elsevier Masson SAS. All rights reserved.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
