New 2H-chromene-3-carboxamide derivatives: Design, synthesis and use as inhibitors of hMAO

…, YY Chen, WJ Tang, JB Shi, YL Tang, BA Song…

Index: Pan, Zhi-Xiang; He, Xu; Chen, Yan-Yan; Tang, Wen-Jian; Shi, Jing-Bo; Tang, Yu-Lan; Song, Bao-An; Li, Jun; Liu, Xin-Hua European Journal of Medicinal Chemistry, 2014 , vol. 80, p. 278 - 284

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Citation Number: 13

Abstract

Abstract A series new 2H-chromene-3-carboxamide derivatives 4a–4t were synthesized and evaluated as monoamine oxidase A and B (MAO-A and MAO-B) inhibitors. Among them, compound 4d (IC 50= 0.93 μM, IC 50 iproniazid= 7.80 μM) showed the most activity and higher MAO-B selectivity (64.5-fold vs. 1-fold) with respect to the MAO-A isoform. The active compound 4d was also docked into the hMAO-B complex structure active site to determine ...