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

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• 作者：Franco Chimenti ; Simone Carradori ; Daniela Secci ; Adriana Bolasco ; Bruna Bizzarri ; Paola Chimenti ; Arianna Granese ; Matilde Yá ; ñ ; ez ; Francisco Orallo
• 关键词：Pyrazoline ; hMAO inhibitors ; Parkinson's disease ; N-Thiocarbamoyl
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：February 2010
• 年：2010
• 卷：45
• 期：2
• 页码：800-804
• 全文大小：199 K

文摘

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.