Affordable Access

Monoamine Oxidase Inhibitory Properties of Optical Isomers and N-substituted Derivatives of 4-methylthioamphetamine

Authors
Publisher
Taylor & Francis Ltd
Publication Date
Keywords
  • Monoamine Oxidase
  • 4-Methylthioamphetamine
  • Mao Inhibitors
  • Amphetamine Derivatives
  • Structure–Activity Relationships
  • Antidepressants
Disciplines
  • Biology

Abstract

(6)-4-Methylthioamphetamine (MTA) was resolved into its enantiomers, and a series of N-alkyl derivatives of the parent compound, as well as its a-ethyl analogue, were prepared. The monoamine oxidase (MAO) inhibitory properties of these substances were evaluated in vitro, using a crude rat brain mitochondrial suspension as the source of enzyme. All compounds produced a selective, reversible and concentration-related inhibition of MAO-A. (1)-MTA proved to be the most potent inhibitor studied, while all the other derivatives were less active than the parent compound, with (2)-MTA being about 18 times less potent than the (1) isomer. The analysis of structure–activity relationships indicates that the introduction of alkyl substituents on the amino group of MTA leads to a reduction in the potency of the derivatives as MAO-A inhibitors, an effect which increases with the size of the substituent.

There are no comments yet on this publication. Be the first to share your thoughts.

Statistics

Seen <100 times
0 Comments

More articles like this

Monoamine oxidase inhibitory properties of optical...

on Journal of enzyme inhibition a... August 2003

Synthesis of substituted benzylidinohydrazines and...

on Journal of Pharmaceutical Scie... January 1975

Effect of quinazolone ring substitution on the mon...

on The Indian Journal of Medical... February 1969

Synthesis of substituted cinnamides: relationship...

on Journal of Pharmaceutical Scie... December 1973
More articles like this..