4.7 Article

Novel Reversible Monoamine Oxidase A Inhibitors: Highly Potent and Selective 3-(1H-Pyrrol-3-yl)-2-oxazolidinones

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 54, Issue 23, Pages 8228-8232

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jm201011x

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Funding

  1. Italian MIUR (Minister dell'Istruzione, dell'Universita e della Ricerca)
  2. Istituto Superiore di Sanita Italy-USA
  3. Istituto Pasteur-Fondazione Cenci Bolognetti
  4. MIUR-PRIN
  5. Fondazione Enrico ed Enrica Sovena

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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 I nM, respectively, 4c being 200000-fold selective for MAO-A with respect to MAO-B.

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