(R)(+)-N-propargyl-1-aminoindan (rasagiline) and derivatives: highly selective and potent inhibitors of monoamine oxidase B.
(+)-N-Propargyl-1-aminoindan (rasagiline) and a series of derivatives have been synthesized and screened for monoamine oxidase inhibitory activity. Rasagiline and several analogues were found be highly selective and potent inhibitors of the B form of the enzyme in contrast to the levorotatory enantiomer which was not active. The results indicate that rasagiline has potential for the treatment of Parkinson's Disease. This compound is currently under development for that indication.
Sterling
J
J
Teva Pharmaceutical Industries, Jerusalem, Israel.
Veinberg
A
A
Lerner
D
D
Goldenberg
W
W
Levy
R
R
Youdim
M
M
Finberg
J
J
D000818:Animals; D001921:Brain / Q000201:enzymology*; D007189:Indans / Q000494:pharmacology*; D007527:Isoenzymes / Q000037:antagonists & inhibitors*; D007700:Kinetics; D008995:Monoamine Oxidase / Q000378:metabolism*; D008996:Monoamine Oxidase Inhibitors / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
D007189:Indans; D007527:Isoenzymes; D008996:Monoamine Oxidase Inhibitors; C031967:rasagiline; D008995:Monoamine Oxidase