New 2-[(5-methoxy-1-methylindolyl)]-alkylamine derivatives: the effect of branching and elongation of the side chain on MAO inhibition.
A novel series of previously synthesised 2-[(5-methoxy-1-methylindolyl)]alkylamine derivatives were irreversible and time-dependent mechanism-based inhibitors of MAO. The effect of branching and elongation of the side chain was evaluated on the inhibitory potency towards MAO-A and MAO-B activities. The KI of the reversible step and the kinact of the irreversible one were determined in each case. The results obtained lead to the conclusion that neither the elongation nor the branching of the side chain improve the potency of the compounds as MAO inhibitors.
Morón
J A
JA
Departament de Bioquímica i Biologia Molecular, Universitat Autònoma de Barcelona, Bellaterra, Spain.
Perez
V
V
Marco
J L
JL
Fernandez-Alvarez
E
E
Unzeta
M
M
D000588:Amines / Q000737:chemistry*; D000818:Animals; D001596:Benzylamines / Q000378:metabolism; D020128:Inhibitory Concentration 50; D007527:Isoenzymes; D007735:Kynuramine / Q000378:metabolism; D008297:Male; D008930:Mitochondria, Liver / Q000201:enzymology; D008995:Monoamine Oxidase / Q000187:drug effects; D008996:Monoamine Oxidase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship; D013997:Time Factors
D000588:Amines; D001596:Benzylamines; D007527:Isoenzymes; D008996:Monoamine Oxidase Inhibitors; D007735:Kynuramine; C030796:benzylamine; D008995:Monoamine Oxidase