Novel Reversible Monoamine Oxidase A Inhibitors: Highly Potent and Selective 3-(1H-Pyrrol-3-yl)-2-oxazolidinones
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- 作者：Sergio Valente ; Stefano Tomassi ; Giampiero Tempera ; Stefania Saccoccio ; Enzo Agostinelli ; Antonello Mai
- 刊名：Journal of Medicinal Chemistry
- 出版年：2011
- 出版时间：December 8, 2011
- 年：2011
- 卷：54
- 期：23
- 页码：8228-8232
- 全文大小：206K
- 年卷期：v.54,no.23(December 8, 2011)
- ISSN：1520-4804
文摘
Monoamine oxidases (MAOs) are involved in various psychiatric and neurodegenerative disorders; hence, MAO inhibitors are useful agents in the therapy of Parkinson鈥檚 disease, Alzheimer鈥檚 dementia, and depression syndrome. Herein we report a novel series of 3-(1H-pyrrol-3-yl)-2-oxazolidinones 3鈥?b>7 as reversible, highly potent and selective anti-MAO-A agents. In particular, 4b, 5b, and 4c showed a Ki-MAO-A of 0.6, 0.8, and 1 nM, respectively, 4c being 200000-fold selective for MAO-A with respect to MAO-B.