Discovery of a 1,2-bis(3-indolyl)ethane that selectively inhibits the pyruvate kinase of methicillin-resistant Staphylococcus aureus over human isoforms

被引：16
|
作者：
Zoraghi, Roya [1 ]
Campbell, Sara [3 ]
Kim, Catrina [3 ]
Dullaghan, Edie M. [3 ]
Blair, Lachlan M. [4 ]
Gillard, Rachel M. [4 ]
Reiner, Neil E. [1 ,2 ]
Sperry, Jonathan [4 ]
机构：
[1] Univ British Columbia, Dept Med, Div Infect Dis, Vancouver, BC V5Z 3J5, Canada
[2] Univ British Columbia, Dept Microbiol & Immunol, Vancouver, BC V5Z 3J5, Canada
[3] Ctr Drug Res & Dev, Vancouver, BC, Canada
[4] Univ Auckland, Sch Chem Sci, Auckland 1, New Zealand
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 21期
关键词：
Pyruvate kinase; MRSA; Antibacterial; Indole; OPTIMIZATION;
D O I：
10.1016/j.bmcl.2014.09.010
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Methicillin-resistant Staphylococcus aureus pyruvate kinase (MRSA PK) has recently been identified as a target for development of novel antibacterial agents. Testing a series of 1,2-bis(3-indolyl)ethanes against MRSA PK has led to the discovery of a potent inhibitor that is selective over human isoforms. (C) 2014 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5059 / 5062
页数：4
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