Symmetrical and unsymmetrical analogues of isoxyl;: active agents against Mycobacterium tuberculosis

被引：40

作者：

Bhowruth, Veemal

Brown, Alistair K.

Reynolds, Robert C.

Coxon, Geoffrey D.

Mackay, Simon P.

Minnikin, David E.

Besra, Gurdyal S. ^{[1
]}

机构：

[1] Univ Birmingham, Sch Biosci, Birmingham B15 2TT, W Midlands, England

[2] So Res Inst, Drug Discovery Div, Birmingham, AL 35225 USA

[3] Univ Strathclyde, Div Pharmaceut Sci, Glasgow G4 0NR, Lanark, Scotland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 18期

基金：

英国医学研究理事会;

关键词：

Mycobacterium tuberculosis; Mt; Mycobacterium bovis; Mb; mycolic acids; isoxyl; inhibitor;

D O I：

10.1016/j.bmcl.2006.06.095

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Symmetrical and unsymmetrical analogues of the antimycobacterial agent isoxyl-have been synthesized and tested against Mycobacterium tuberculosis H37Rv and Mycobacterium bovis BCG, some showing an increased bactericidal effect. In particular, compounds 1-(p-n-butylphenyl)-3-(4-propoxy-phenyl) thiourea (10) and 1-(p-n-butylphenyl)-3-(4-n-butoxy-phenyl) thiourea (11) showed an approximate 10-fold increase in in vitro potency compared to isoxyl, paralleled by increased inhibition of mycolic acid biosynthesis in M. bovis BCG. Interestingly, these isoxyl analogues showed relatively poor inhibition of oleate production, suggesting that the modifications have changed the spectrum of biological activity. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：4743 / 4747

页数：5

共 17 条

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