Novel tricyclic pyrazolo[1,5-d][1,4]benzoxazepin-5(6H)-one: Design, synthesis, model and use as hMAO-B inhibitors.

Rui Chen,Jie Xiao,Yong Ni,Han-Fei Xu,Min Zheng,Xu Tong,Tong-Tian Zhang,Chenzhong Liao,Wen-Jian Tang

Bioorganic & Medicinal Chemistry（2016）

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摘要

Novel tricyclic pyrazolo[1,5-d][1,4]benzoxazepin-5(6H)-one as potential selective hMAO-B inhibitors were designed and synthesized. Modeling study indicated that the hMAO-B selectivity is determined by at least two residues, i.e., Ile 199 and Cys 172.

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关键词

hMAO,Isoform selectivity,Benzoxazepinone,Selective hMAO-B inhibitor,Anti-Parkinson

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