Inhibitory potency of some isatin analogues on human monoamine oxidase A and B.
Isatin is an endogenous compound which acts as a selective inhibitor of monoamine oxidase (MAO) B. In this study a range of isatin analogues were tested for their in vitro inhibition of human MAO A and B. Most of the analogues were less potent than isatin. Hydroxylation of the aromatic ring changed the inhibitory potency in favour of MAO A, with 5-hydroxyisatin being a potent and selective MAO A inhibitor (IC50 8 microM). Isatinic acid, which is formed reversibly from isatin at alkaline pH, showed no inhibition.
Medvedev
A E
AE
Institute of Biological and Medical Chemistry, Academy of Medical Sciences, Moscow, Russia.
Goodwin
B
B
Clow
A
A
Halket
J
J
Glover
V
V
Sandler
M
M
D001792:Blood Platelets / Q000187:drug effects; D006801:Humans; D006863:Hydrogen-Ion Concentration; D006900:Hydroxylation; D007510:Isatin / Q000031:analogs & derivatives* / Q000494:pharmacology; D008995:Monoamine Oxidase / Q000378:metabolism; D008996:Monoamine Oxidase Inhibitors / Q000494:pharmacology*; D010920:Placenta / Q000187:drug effects
D008996:Monoamine Oxidase Inhibitors; D007510:Isatin; D008995:Monoamine Oxidase