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 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.
Novel reversible monoamine oxidase A inhibitors: highly potent and selective 3-(1H-pyrrol-3-yl)-2-oxazolidinones / Valente, S; Tomassi, S; Tempera, G; Saccoccio, S; Agostinelli, E; Mai, A. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 1520-4804. - 54:23(2011), pp. 8228-8232.
Novel reversible monoamine oxidase A inhibitors: highly potent and selective 3-(1H-pyrrol-3-yl)-2-oxazolidinones
Tomassi SSecondo
Membro del Collaboration Group
;
2011
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 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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
