Synthesis and Evaluation of Potent Ene-yne Inhibitors of Type II Dehydroquinases as Tuberculosis Drug Leads

被引：12

作者：

Anh Thu Tran

Cergol, Katie M.

West, Nicholas P. ^{[1
,2
]}

Randall, Elizabeth J. ^{[1
,2
]}

Britton, Warwick J. ^{[1
,2
]}

Bokhari, Syed Ali Imran ^{[3
,4
]}

Ibrahim, Musadiq ^{[3
,4
]}

Lapthorn, Adrian J. ^{[3
,4
]}

Payne, Richard J.

机构：

[1] Centenary Inst Canc Med & Cell Biol, Mycobacterial Res Program, Sydney, NSW, Australia

[2] Univ Sydney, Sydney Med Sch, Sydney, NSW 2006, Australia

[3] Univ Glasgow, Dept Chem, Glasgow G12 8QQ, Lanark, Scotland

[4] Univ Glasgow, Div Biochem & Life Sci, Glasgow G12 8QQ, Lanark, Scotland

来源：

CHEMMEDCHEM | 2011年 / 6卷 / 02期

基金：

英国医学研究理事会;

关键词：

antibiotics; dehydroquinases; medicinal chemistry; Mycobacterium tuberculosis; shikimate pathway; NANOMOLAR COMPETITIVE INHIBITORS; ALAMAR BLUE ASSAY; MYCOBACTERIUM-TUBERCULOSIS; BIOLOGICAL EVALUATION; HELICOBACTER-PYLORI; SHIKIMATE PATHWAY; STREPTOMYCES-COELICOLOR; STEREOCHEMICAL COURSES; DESIGN; 3-DEHYDROQUINASES;

D O I：

10.1002/cmdc.201000399

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

E-9: You sunk my battleship! Potent ene-yne-based inhibitors of typeII dehydroquinase are described. The majority of the compounds exhibited nanomolar inhibition of the Streptomyces coelicolor, Helicobacter pylori and Mycobacterium tuberculosis typeII dehydroquinases. The inhibitors also possessed moderate activity against the growth of M.tuberculosis in vitro. © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

引用

收藏

页码：262 / 265

页数：4

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