Structure-activity relationships of 2-aryl-1H-indole inhibitors of the NorA efflux pump in Staphylococcus aureus

被引：69

作者：

Ambrus, Joseph I. ^{[1
]}

Kelso, Michael J. ^{[1
]}

Bremner, John B. ^{[1
]}

Ball, Anthony R. ^{[2
]}

Casadei, Gabriele ^{[2
]}

Lewis, Kim ^{[2
]}

机构：

[1] Univ Wollongong, Sch Chem, Wollongong, NSW 2522, Australia

[2] Northeastern Univ, Dept Biol & Antimicrobial Discovery Ctr, Boston, MA 02115 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 15期

关键词：

2-arylindoles; NorA efflux pump inhibitors; antibacterial;

D O I：

10.1016/j.bmcl.2008.06.093

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of 22 2-aryl-1H-indoles, including 12 new compounds, has been achieved via Pd- or Rh-mediated methodologies, or selective electrophilic substitution. All three methods were based on elaborations from simple indole precursors. SAR studies on these indoles and 2-phenyl-1H-indole in Staphylococcus aureus as NorA efflux pump inhibitors indicated 5-nitro-2-(3-methoxycarbonyl)phenyl-1H-indole was a slightly more potent inhibitor than the lead INF55. A promising new antibacterial lead compound against S. aureus (2-phenyl-1H-indol-5-yl)-methanol, was also found. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：4294 / 4297

页数：4

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