1214740-86-9Relevant academic research and scientific papers
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,Granese, Arianna,Yá?ez, Matilde,Orallo, Francisco
, p. 800 - 804 (2010)
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 IC50 2.75 ± 0.81 μM value and selectivity ratio of 25, which is the best candidate for further investigations.
