Design and synthesis of novel chalcones as potent selective monoamine oxidase-B inhibitors

被引：76

作者：

Hammuda, Arwa ^{[1
]}

Shalaby, Raed ^{[1
]}

Rovida, Stefano ^{[2
]}

Edmondson, Dale E. ^{[3
]}

Binda, Claudia ^{[2
]}

Khalil, Ashraf ^{[1
]}

机构：

[1] Qatar Univ, Coll Pharm, POB 2713, Doha, Qatar

[2] Univ Pavia, Dept Biol & Biotechnol, Via Ferrata 1, I-27100 Pavia, Italy

[3] Emory Univ, Sch Med, Dept Biochem, Atlanta, GA 30322 USA

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2016年 / 114卷

关键词：

Monoamine oxidase; Neuroprotection; Drug design; Synthesis; Enzyme; Chalcones; BIOLOGICAL EVALUATION; DERIVATIVES; SAFINAMIDE; SERIES;

D O I：

10.1016/j.ejmech.2016.02.038

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of substituted chalcones were designed and synthesized to be evaluated as selective human MAO-B inhibitors. A combination of either methylsulfonyl or trifluoromethyl substituents on the aromatic ketone moiety with a benzodioxol ring on the other end of the chalcone scaffold was investigated. The compounds were tested for their inhibitory activities on both human MAO-A and B. All compounds appeared to be selective MAO-B inhibitors with K-i values in the micromolar to sub-micromolar range. Molecular modeling studies have been performed to get insight into the binding mode of the synthesized compounds to human MAO-B active site. (C) 2016 Elsevier Masson SAS. All rights reserved.

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收藏

页码：162 / 169

页数：8

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