Novel anti-infection agents: Small-molecule inhibitors of bacterial transcription factors

被引：45
|
作者：
Bowser, Todd E.
Bartlett, Victoria J.
Grier, Mark C.
Verma, Atul K.
Warchol, Taduesz
Levy, Stuart B.
Alekshun, Michael N.
机构：
[1] Paratek Pharmaceut Inc, Boston, MA 02111 USA
[2] Tufts Univ, Sch Med, Ctr Adaptat Genet & Drug Resistance, Boston, MA 02111 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 20期
关键词：
antibacterials; virulence; hydroxybenzamidazoles; transcription;
D O I：
10.1016/j.bmcl.2007.07.072
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Structure-based drug design was utilized to identify potent small-molecule inhibitors of proteins within the AraC family of bacterial transcription factors, which control virulence in medically important microbes. These agents represent a novel approach to fight infectious disease and may be less likely to promote resistance development. These compounds lack intrinsic antibacterial activity in vitro and were able to limit a bacterial infection in a mouse model of urinary tract infection. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5652 / 5655
页数：4
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