Inhibitory potency of some isatin analogues on human monoamine oxidase A and B

  • Biochem Pharmacol. 1992 Aug 4;44(3):590-2. doi: 10.1016/0006-2952(92)90454-q.
A E Medvedev  1 ,  B Goodwin ,  A Clow ,  J Halket ,  V Glover ,  M Sandler
Affiliations
  • 1. Institute of Biological and Medical Chemistry, Academy of Medical Sciences, Moscow, Russia.
PMID: 1510706 DOI: 10.1016/0006-2952(92)90454-q
Abstract

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.

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