1,3,4-Oxadiazole-3(2H)-carboxamide derivatives as potential novel class of monoamine oxidase (MAO) inhibitors: Synthesis, evaluation, and role of urea moiety

Shaoyong Ke, Zhong Li, Xuhong Qian*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

32 Scopus citations

Abstract

A new series of 1,3,4-oxadiazole-3(2H)-carboxamide derivatives have been synthesized by direct heterocyclization reaction of substituted benzoylisocyanate with various aroylhydrazones as novel monoamine oxidase inhibitors (MAOIs). The target molecules have been identified on the basis of satisfactory analytical and spectra (IR, 1H NMR, 13C NMR, and HR-MS) data. The newly synthesized compounds were evaluated for their MAO inhibitory activity by kynuramine fluorimetric assay method. The preliminary results showed that most of the compounds have moderate inhibitory activities toward MAO at the concentration of 10-5-10-3 M. This work may provide a novel class of lead compounds with potential MAO inhibitions for further optimization.

Original languageEnglish
Pages (from-to)7565-7572
Number of pages8
JournalBioorganic and Medicinal Chemistry
Volume16
Issue number16
DOIs
StatePublished - 15 Aug 2008
Externally publishedYes

Keywords

  • 1,3,4-Oxadiazole-3(2H)-carboxamide
  • Heterocycle
  • MAO inhibitor
  • Urea

Fingerprint

Dive into the research topics of '1,3,4-Oxadiazole-3(2H)-carboxamide derivatives as potential novel class of monoamine oxidase (MAO) inhibitors: Synthesis, evaluation, and role of urea moiety'. Together they form a unique fingerprint.

Cite this