期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 54, 期 23, 页码 8228-8232出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm201011x
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资金
- Italian MIUR (Minister dell'Istruzione, dell'Universita e della Ricerca)
- Istituto Superiore di Sanita Italy-USA
- Istituto Pasteur-Fondazione Cenci Bolognetti
- MIUR-PRIN
- Fondazione Enrico ed Enrica Sovena
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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