Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur, Fondazione Cenci Bolognetti, Sapienza Università di Roma, Piazzale Aldo Moro 5, 00185 Roma, Italy.
J Med Chem. 2011 Dec 8;54(23):8228-32. doi: 10.1021/jm201011x. Epub 2011 Nov 7.
Monoamine oxidases (MAOs) are involved in various psychiatric and neurodegenerative disorders; hence, MAO inhibitors are useful agents in the therapy of Parkinson's disease, Alzheimer's dementia, and depression syndrome. Herein we report a novel series of 3-(1H-pyrrol-3-yl)-2-oxazolidinones 3-7 as reversible, highly potent and selective anti-MAO-A agents. In particular, 4b, 5b, and 4c showed a K(i-MAO-A) of 0.6, 0.8, and 1 nM, respectively, 4c being 200000-fold selective for MAO-A with respect to MAO-B.
单胺氧化酶（MAOs）参与多种精神疾病和神经退行性疾病；因此，MAO 抑制剂是治疗帕金森病、阿尔茨海默病痴呆和抑郁症的有效药物。本文报道了一系列新型 3-(1H-吡咯-3-基)-2-恶唑烷酮 3-7，它们是可逆的、高活性和选择性的 MAO-A 抑制剂。特别是，化合物 4b、5b 和 4c 的 MAO-A 抑制常数（K(i-MAO-A)）分别为 0.6、0.8 和 1 nM，4c 对 MAO-A 的选择性是 MAO-B 的 200000 倍。
