Design, synthesis, and in vitro hMAO-B inhibitory evaluation of some 1-methyl-3,5-diphenyl-4,5-dihydro-1H-pyrazoles

详细信息    查看全文

• 作者：Rossella Fioravanti ; Nicoletta Desideri ; Mariangela Biava ; Luca Proietti Monaco ; Laura Grammatica ; Matilde Y¨¢?ez
• 关键词：Pyrazole derivatives ; Monoamine oxidases ; hMAO inhibitors
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2013
• 出版时间：15 September, 2013
• 年：2013
• 卷：23
• 期：18
• 页码：5128-5130
• 全文大小：383 K

文摘

A series of 1-methyl-3,5-diphenyl-4,5-dihydro-1H-pyrazoles (3a-k and 4a-u) were designed, synthesized, and evaluated for their inhibitory efficacy towards the two hMAO isoforms. Most of the derivatives were found to be potent and selective hMAO-B inhibitors. In particular, derivative 3g showed greater hMAO-B affinity than selective inhibitor selegiline coupled with high selectivity index (SI = 145). The most selective hMAO-B inhibitor was the 3-methyl analogue 3f with an SI higher than 909.