异噁唑的对称和不对称类似物；抗结核分枝杆菌的活性剂。
Symmetrical and unsymmetrical analogues of isoxyl; active agents against Mycobacterium tuberculosis.
作者信息
Bhowruth Veemal, Brown Alistair K, Reynolds Robert C, Coxon Geoffrey D, Mackay Simon P, Minnikin David E, Besra Gurdyal S
机构信息
School of Biosciences, University of Birmingham, Edgbaston, Birmingham B15 2TT, UK.
出版信息
Bioorg Med Chem Lett. 2006 Sep 15;16(18):4743-7. doi: 10.1016/j.bmcl.2006.06.095. Epub 2006 Jul 27.
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.
已合成抗分枝杆菌药物异烟肼的对称和不对称类似物，并针对结核分枝杆菌H37Rv和牛分枝杆菌卡介苗进行了测试，其中一些显示出增强的杀菌效果。特别是，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)与异烟肼相比，体外效力提高了约10倍，同时牛分枝杆菌卡介苗中分枝菌酸生物合成的抑制作用增强。有趣的是，这些异烟肼类似物对油酸生成的抑制作用相对较弱，这表明这些修饰改变了生物活性谱。
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