Abstract
Novel 1-(4-arylthiazol-2-yl)-2-(3-methylcyclohexylidene)hydrazine derivatives have been investigated for their ability to inhibit selectively the activity of the human B isoform of monoamine oxidase. These compounds were obtained as racemates and (R)-enantiomers by a stereoconservative synthetic pattern in high yield and enantiomeric excess. The (S)-enantiomers of the most active derivatives have been separated by enantioselective HPLC. All compounds showed selective activity against hMAO-B with IC(50) ranging between 21.90 and 0.018 microM.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Chromatography, High Pressure Liquid
-
Cyclohexanes / chemical synthesis*
-
Cyclohexanes / chemistry
-
Cyclohexanes / isolation & purification
-
Humans
-
Hydrazines / chemical synthesis*
-
Hydrazines / chemistry
-
Hydrazines / isolation & purification
-
Isoenzymes / antagonists & inhibitors
-
Isoenzymes / chemistry
-
Monoamine Oxidase / chemistry*
-
Monoamine Oxidase Inhibitors / chemical synthesis*
-
Monoamine Oxidase Inhibitors / chemistry
-
Monoamine Oxidase Inhibitors / isolation & purification
-
Stereoisomerism
-
Structure-Activity Relationship
-
Triazoles / chemical synthesis*
-
Triazoles / chemistry
-
Triazoles / isolation & purification
Substances
-
Cyclohexanes
-
Hydrazines
-
Isoenzymes
-
Monoamine Oxidase Inhibitors
-
Triazoles
-
Monoamine Oxidase