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Novel reversible monoamine oxidase A inhibitors: highly potent and selective 3-(1H-pyrrol-3-yl)-2-oxazolidinones.

Abstract : 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.
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Submitted on : Thursday, April 17, 2014 - 3:34:08 PM
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Sergio Valente, Stefano Tomassi, Giampiero Tempera, Stefania Saccoccio, Enzo Agostinelli, et al.. Novel reversible monoamine oxidase A inhibitors: highly potent and selective 3-(1H-pyrrol-3-yl)-2-oxazolidinones.. Journal of Medicinal Chemistry, American Chemical Society, 2011, 54 (23), pp.8228-32. ⟨10.1021/jm201011x⟩. ⟨pasteur-00980200⟩



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