Monoamine oxidase inhibitor properties of some benzazoles: structure-activity relationships

AAPS PharmSci. 1999;1(4):E16. doi: 10.1208/ps010416.

Abstract

Benzazoles containing two or three nitrogen atoms were screened for their inhibitory activity toward monoamine oxidases MAO-A and MAO-B. In order to clarify the mechanism of interaction of these compounds with the enzyme, their electronic structure was calculated at the ab initio level and the influence of lipophilicity on activity was investigated. The mode of binding of benzazoles to MAO-B appears different from that of previously investigated heterocycles.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzimidazoles / chemistry
  • Benzimidazoles / pharmacology*
  • Drug Evaluation, Preclinical
  • In Vitro Techniques
  • Indazoles / chemistry
  • Indazoles / pharmacology*
  • Monoamine Oxidase / metabolism*
  • Monoamine Oxidase Inhibitors / chemistry
  • Monoamine Oxidase Inhibitors / pharmacology*
  • Rats
  • Structure-Activity Relationship
  • Triazoles / chemistry
  • Triazoles / pharmacology*

Substances

  • Benzimidazoles
  • Indazoles
  • Monoamine Oxidase Inhibitors
  • Triazoles
  • Monoamine Oxidase