Inhibition of monoamine oxidase - A activity in rat brain by synthetic hydrazines: Structure-activity relationship (SAR)

Ahsana Dar, Khalid M. Khan, Humayun S. Ateeq, Shagufta Khan, Shagufta Rahat, Shahnaz Perveen, Claudiu T. Supuran

Research output: Contribution to journalArticlepeer-review

24 Citations (Scopus)

Abstract

A series of hydrazine derivatives was synthesized in order to evaluate their monoamine oxidase A (MAO-A) inhibitory effects. MAO-A inhibitory activity of 4-tosyl benzoic acid carbohydrazide was quite potent, similarly to that of the corresponding 4-benzyloxy-benzoic acid carbohydrazide and its N-cyanoethylated derivative. Structural variations of these compounds, such as the replacement of the 4-substitutent, of the aromatic ring on which the carbohydrazide moiety is grafted, as well as cyclization of the hydrazide moiety in five- or six-membered rings caused either significant decline or complete loss of MAO inhibitory properties. The most active compound (4-tosyl benzoic acid carbohydrazide) was also subjected to the forced swim test, an animal model of depression, eliciting a marked reduction in immobility time in rats, without affecting the locomotor activity, implying that it possesses anti-depressant properties due to inhibition of MAO type-A.

Original languageEnglish
Pages (from-to)269-274
Number of pages6
JournalJournal of Enzyme Inhibition and Medicinal Chemistry
Volume20
Issue number3
DOIs
Publication statusPublished - Jun 2005

Keywords

  • Hydrazides
  • Inhibition
  • MAO-A
  • Monoamine oxidase-A
  • Rat brain
  • Structure activity

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