1, 5-Diphenylpenta-2, 4-dien-1-ones as potent and selective monoamine oxidase-B inhibitors

N Desideri, R Fioravanti, LP Monaco, M Biava…

Index: Desideri, Nicoletta; Fioravanti, Rossella; Proietti Monaco, Luca; Biava, Mariangela; Yanez, Matilde; Ortuso, Francesco; Alcaro, Stefano European Journal of Medicinal Chemistry, 2013 , vol. 59, p. 91 - 100

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Citation Number: 9

Abstract

A series of (2E, 4E)-1-(2-hydroxyphenyl)-5-phenylpenta-2, 4-dien-1-ones (3a–r) and (2Z, 4E)-3-hydroxy-1-(2-hydroxyphenyl)-5-phenylpenta-2, 4-dien-1-ones (6a–l) were synthesized and evaluated in vitro as inhibitors of the two human Monoamine oxidase (hMAO) isoforms, MAO-A and MAO-B. Most of the compounds showed a selective MAO-B inhibitory activity in the nanomolar or low micromolar range.(2E, 4E)-5-(4-Chlorophenyl)-1 ...