Design, synthesis and antibacterial activities of thiouracil derivatives containing acyl thiourea as SecA inhibitors

被引：33

作者：

Cui, Penglei ^{[1
,2
]}

Li, Xiaoliu ^{[1
]}

Zhu, Mengyuan ^{[3
,4
]}

Wang, Binghe ^{[3
,4
]}

Liu, Jing ^{[5
]}

Chen, Hua ^{[1
]}

机构：

[1] Hebei Univ, Coll Chem & Environm Sci, Key Lab Chem Biol Hebei Prov, Baoding 071002, Peoples R China

[2] Agr Univ Hebei, Coll Sci, Baoding 071001, Peoples R China

[3] Georgia State Univ, Dept Chem, Atlanta, GA 30302 USA

[4] Georgia State Univ, Ctr Diagnost & Therapeut, Atlanta, GA 30302 USA

[5] Agr Univ Hebei, Coll Vet Med, Baoding 071001, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2017年 / 27卷 / 10期

关键词：

SecA inhibitors; Antibacterial activity; Molecular simulation; Thiouracil; Acyl thiourea; BACTERIAL PROTEIN SECRETION; BIOLOGICAL EVALUATION; MOLECULAR DOCKING; ANALOGS; TRANSLOCATION;

D O I：

10.1016/j.bmcl.2016.11.060

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel thiouracil derivatives containing an acyl thiourea moiety (7a-7x) have been synthesized by structural modification of a lead SecA inhibitor, 2. All the compounds have been evaluated for their antibacterial activities against Bacillus amyloliquefaciens, Staphylococcus aureus, and Bacillus subtilis. Compounds 7c, 7m, 7u, 7v exhibited promising activities against above bacteria. Such four compounds were further tested for their inhibitory activity against SecA ATPase, and the results showed that compounds 7c and 7u had higher inhibitory activities than that of compound 2. Molecular docking work suggests that compound 7u might bind at a pocket close to the ATPase ATP-binding domain. (C) 2016 Elsevier Ltd. All rights reserved.

引用

页码：2234 / 2237

页数：4

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