Design, synthesis, and structural studies on potent biaryl inhibitors of type II dehydroquinases

被引：22

作者：

Payne, Richard J.

Riboldi-Tunnicliffe, Alan

Kerbarh, Olivier

Abell, Andrew D.

Lapthorn, Adrian J.

Abell, Chris

机构：

[1] Department of Chemistry, University of Cambridge, CB2 1EW, Cambridge, Lensfield Road

[2] Department of Chemistry, Division of Biochemistry and Life Sciences, University of Glasgow, Glasgow

[3] Department of Chemistry, University of Canterbury, Christchurch

来源：

CHEMMEDCHEM | 2007年 / 2卷 / 07期

基金：

英国生物技术与生命科学研究理事会;

关键词：

D O I：

10.1002/cmdc.200700062

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Filling the pocket: Biaryl inhibitors of type II dehydroquinase are described, designed to bind to both the active site and a subsidiary pocket. Compounds exhibited nanomolar inhibition of the enzyme, which is rationalised by molecular docking and protein crystallographic studies. (Figure Presented) © 2007 Wiley-VCH Verlag GmbH & Co. KGaA.

引用

页码：1010 / 1013

页数：4

共 17 条

[1]

Abell C., 1999, ENZYMOLOGY MOL BIOL, P573

[2]

[Anonymous], BIOSYNTHESIS AROMATI

[3] Cloning, sequencing, expression, purification and preliminary characterization of a type II dehydroquinase from Helicobacter pylori [J].