Symmetrical and unsymmetrical analogues of isoxyl;: active agents against Mycobacterium tuberculosis
Symmetrical and unsymmetrical analogues of isoxyl;: active agents against Mycobacterium tuberculosis
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DOI：
10.1016/j.bmcl.2006.06.095
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发表时间：
2006-09-15
影响因子：
2.7
通讯作者：
Besra, Gurdyal S.
中科院分区：
文献类型：
--
作者：
Bhowruth, Veemal;Brown, Alistair K.;Besra, Gurdyal S.
已合成了抗分枝杆菌剂Islam的对称和不对称类似物，并对结核分枝杆菌H37 Rv和牛分枝杆菌BCG进行了测试，其中一些显示出增强的杀菌效果。具体地说，化合物1-（对正丁基苯基）-3-（4-丙氧基苯基）硫脲（10）和1-（对正丁基苯基）-3-（4-正丁氧基苯基）硫脲（11）显示出与isoxyl相比体外效力增加约10倍，这是由于增加了对分枝菌中分枝菌酸生物合成的抑制。牛卡介苗有趣的是，这些isoxyl类似物显示出相对较差的抑制油酸生产，这表明修饰改变了生物活性谱。(c)2006爱思唯尔有限公司保留所有权利。
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.