Structure-based design, synthesis and A-site rRNA co-crystal complexes of novel amphiphilic aminoglycoside antibiotics with new binding modes: A synergistic hydrophobic effect against resistant bacteria

被引：31

作者：

Hanessian, Stephen ^{[1
]}

Pachamuthu, Kandasamy ^{[1
]}

Szychowski, Janek ^{[1
]}

Giguere, Alexandre ^{[1
]}

Swayze, Eric E. ^{[2
]}

Migawa, Michael T. ^{[2
]}

Francois, Boris ^{[3
]}

Kondo, Jiro ^{[3
,4
]}

Westhof, Eric ^{[3
]}

机构：

[1] Univ Montreal, Dept Chem, Montreal, PQ H3C 3J7, Canada

[2] ISIS Pharmaceut, Carlsbad, CA 92008 USA

[3] Univ Strasbourg, CNRS, IBMC, Architecture & React ARN, F-67084 Strasbourg, France

[4] Sophia Univ, Fac Sci & Technol, Dept Mat & Life Sci, Chiyoda Ku, Tokyo 1028554, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 23期

基金：

加拿大自然科学与工程研究理事会;

关键词：

Antibiotic resistance; Aminoglycoside; RNA-complex; DECODING SITE; ANTIBACTERIAL ACTIVITIES; PAROMOMYCIN; DERIVATIVES; ANALOGS;

D O I：

10.1016/j.bmcl.2010.09.084

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Incorporation of an hydrophobic (phenethylamino) ethyl ether at C2 '' of N1-(HABA)-3',4'-dideoxyparomomycin led to a novel analog with an excellent antibacterial profile against a host of resistant bacteria. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：7097 / 7101

页数：5