Ke Shaoyong, Li Zhong, Qian Xuhong
Shanghai Key Laboratory of Chemical Biology, Institute of Pesticides and Pharmaceuticals, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.
Bioorg Med Chem. 2008 Aug 15;16(16):7565-72. doi: 10.1016/j.bmc.2008.07.026. Epub 2008 Jul 18.
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, (1)H NMR, (13)C 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.
通过取代苯甲酰异氰酸酯与各种芳酰腙的直接杂环化反应,合成了一系列新型的1,3,4-恶二唑-3(2H)-甲酰胺衍生物作为新型单胺氧化酶抑制剂(MAOIs)。根据令人满意的分析和光谱(红外光谱、(1)H核磁共振谱、(13)C核磁共振谱和高分辨质谱)数据确定了目标分子。通过犬尿胺荧光分析法评估了新合成化合物的MAO抑制活性。初步结果表明,大多数化合物在10(-5)-10(-3)M浓度下对MAO具有中等抑制活性。这项工作可能为进一步优化提供一类具有潜在MAO抑制作用的新型先导化合物。