2-and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion

被引：31

作者：

Sayer, James R. ^{[1
]}

Wallden, Karin ^{[2
]}

Pesnot, Thomas ^{[1
]}

Campbell, Frederick ^{[1
]}

Gane, Paul J. ^{[3
]}

Simone, Michela ^{[3
]}

Koss, Hans ^{[1
]}

Buelens, Floris ^{[2
]}

Boyle, Timothy P. ^{[1
]}

Selwood, David L. ^{[3
]}

Waksman, Gabriel ^{[2
]}

Tabor, Alethea B. ^{[1
]}

机构：

[1] UCL, Dept Chem, London WC1H 0AJ, England

[2] UCL & Birkbeck, Inst Struct & Mol Biol, London WC1E 7HX, England

[3] UCL, Wolfson Inst Biomed Res, London WC1E 6BT, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2014年 / 22卷 / 22期

基金：

英国惠康基金; 英国生物技术与生命科学研究理事会;

关键词：

8-Amino imidazo[1,2-a]pyrazine; Bacterial type IV secretion system; HP0525; ATPase inhibitor; DESIGN; DERIVATIVES; AMINATION; SYSTEMS; KINASE; (R)-TEMBAMIDE; CHEMISTRY; DISCOVERY; ALCOHOLS; CATALYST;

D O I：

10.1016/j.bmc.2014.09.036

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A novel series of 8-amino imidazo[1,2-a] pyrazine derivatives has been developed as inhibitors of the VirB11 ATPase HP0525, a key component of the bacterial type IV secretion system. A flexible synthetic route to both 2- and 3-aryl substituted regioisomers has been developed. The resulting series of imidazo[1,2-a] pyrazines has been used to probe the structure-activity relationships of these inhibitors, which show potential as antibacterial agents. (C) 2014 The Authors. Published by Elsevier Ltd.

引用

收藏

页码：6459 / 6470

页数：12

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