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 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.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Animals
-
Cattle
-
In Vitro Techniques
-
Isoenzymes / antagonists & inhibitors
-
Isoenzymes / metabolism
-
Monoamine Oxidase / metabolism*
-
Monoamine Oxidase Inhibitors / chemical synthesis*
-
Monoamine Oxidase Inhibitors / chemistry
-
Monoamine Oxidase Inhibitors / pharmacology
-
Oxazolidinones / chemical synthesis*
-
Oxazolidinones / chemistry
-
Oxazolidinones / pharmacology
-
Pyrroles / chemical synthesis*
-
Pyrroles / chemistry
-
Pyrroles / pharmacology
-
Stereoisomerism
-
Structure-Activity Relationship
Substances
-
Isoenzymes
-
Monoamine Oxidase Inhibitors
-
Oxazolidinones
-
Pyrroles
-
Monoamine Oxidase