Novel Reversible Monoamine Oxidase A Inhibitors: Highly Potent and Selective 3-(1H-Pyrrol-3-yl)-2-oxazolidinones
| Autor: | Stefania Saccoccio, Sergio Valente, Stefano Tomassi, Enzo Agostinelli, Antonello Mai, G. Tempera |
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| Přispěvatelé: | Department of Medicinal Chemistry and Technologies, Institut Pasteur, Fondation Cenci Bolognetti - Istituto Pasteur Italia, Fondazione Cenci Bolognetti, Réseau International des Instituts Pasteur (RIIP)-Réseau International des Instituts Pasteur (RIIP)-Università degli Studi di Roma 'La Sapienza' = Sapienza University [Rome], Department of Biochemical Sciences 'Rossi Fanelli' |
| Rok vydání: | 2011 |
| Předmět: |
Monoamine Oxidase Inhibitors
Monoamine oxidase MESH: Monoamine Oxidase Inhibitors Stereoisomerism In Vitro Techniques Pharmacology MESH: Monoamine Oxidase 01 natural sciences Isozyme Structure-Activity Relationship 03 medical and health sciences MESH: Structure-Activity Relationship MESH: Oxazolidinones Drug Discovery medicine Animals Structure–activity relationship Dementia MESH: Animals [SDV.BBM]Life Sciences [q-bio]/Biochemistry Molecular Biology Pyrroles Monoamine Oxidase Oxazolidinones 030304 developmental biology 0303 health sciences 010405 organic chemistry Chemistry MAO inhibitors medicine.disease MESH: Stereoisomerism Monoamine Oxidase-A Inhibitors 3. Good health 0104 chemical sciences Isoenzymes MESH: Cattle Monoamine neurotransmitter MESH: Isoenzymes MESH: Pyrroles Molecular Medicine Cattle |
| Zdroj: | Journal of Medicinal Chemistry Journal of Medicinal Chemistry, American Chemical Society, 2011, 54 (23), pp.8228-32. ⟨10.1021/jm201011x⟩ |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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