杂环酮腙与类似物的合成及其对结核杆菌的抑制活性  

Synthesis and Anti-mycobacterial Activities of Heterocyclic Hydrazones and Their Bioisosteric Compounds

作　　者：李忠洲[1] 赵升[1] 李新军[1] 王翠翠[1] 姚璐璐[1] 金瑞良[2] 邹新琢[1] 

机构地区：[1]华东师范大学化学系,上海200241 [2]同济大学附属上海肺科医院上海市结核病(肺)重点实验室,上海200433

出　　处：《有机化学》2015年第6期1310-1319,共10页Chinese Journal of Organic Chemistry

摘　　要：22个新的杂环酮腙及其类似物被合成,其对结核分枝杆菌菌株H37Rv的抑菌活性被测定.这些化合物都显示出抑菌活性.其中,化合物(1E,4E)-1,5-二(5'-溴-2'-噻吩基)-1,4-戊二烯-3-酮-(1',4',5',6'-四氢嘧啶基)腙(1d)的MIC90为2μg/m L,显示出最高的抑菌活性;同时该化合物对单耐异烟肼菌株242、耐多药菌株2312和广泛耐药菌株1220的MIC90值分别为0.25,1.0和0.5μg/m L,也表现出很好的抑菌作用.A total of 22 new heterocyclic hydrazones and their bioisosteric compounds were synthesized and evaluated for their activity against Mycobacterium tuberculosis, strain H37 Rv. All newly synthesized compounds showed inhibitory activities. Among these compounds,（1E,4E）-1,5-bis（5-bromo-2-thiophenyl）-1,4-pentadiene-3-one-（1,4,5,6-tetrahydro-2-pyrimidimyl）-hydrazone（1d） showed the most effective anti-tubercular activity with MIC90 value of 2 μg/m L, and exhibited an excellent inhibitory activity against isoniazid-resistant strain 242, multidrug-resistant strain 2312, and extensively drug-resistant strain 1220 with MIC90 values of 0.25, 1.0 and 0.5 μg/m L, respectively.

关 键 词：杂环酮腙 合成 结核分枝杆菌 抑菌活性 

分 类 号：O626[理学—有机化学]