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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*
  • *此作品的通讯作者

科研成果: 期刊稿件文章同行评审

摘要

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.

源语言英语
页(从-至)7565-7572
页数8
期刊Bioorganic and Medicinal Chemistry
16
16
DOI
出版状态已出版 - 15 8月 2008
已对外发布

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