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

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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Field Value
Source ISSN: 0022-2623
Author Valente, Sergio, Tomassi, Stefano, Tempera, Giampiero, Saccoccio, Stefania, Agostinelli, Enzo, Mai, Antonello
Maintainer CCSD
Last Updated May 5, 2026, 14:17 (UTC)
Created May 5, 2026, 14:17 (UTC)
Identifier pasteur-00980200
Language en
Rights https://about.hal.science/hal-authorisation-v1/
contributor Department of Medicinal Chemistry and Technologies ; Institut Pasteur, Fondation Cenci Bolognetti - Istituto Pasteur Italia, Fondazione Cenci Bolognetti ; Pasteur Network (Réseau International des Instituts Pasteur)-Pasteur Network (Réseau International des Instituts Pasteur)-Università degli Studi di Roma "La Sapienza" = Sapienza University [Rome] (UNIROMA)
creator Valente, Sergio
date 2011-12-08T00:00:00
harvest_object_id 4765a4e8-3e35-4c59-b3a7-a432a727fb1f
harvest_source_id 3374d638-d20b-4672-ba96-a23232d55657
harvest_source_title test moissonnage SELUNE
metadata_modified 2025-03-14T00:00:00
relation info:eu-repo/semantics/altIdentifier/doi/10.1021/jm201011x
set_spec type:ART