杂环酮腙与类似物的合成及其对结核杆菌的抑制活性

doi:10.6023/cjoc201412011

摘要/Abstract

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2 μg/mL, 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0.5 μg/mL, 也表现出很好的抑菌作用.

关键词: 杂环酮腙, 合成, 结核分枝杆菌, 抑菌活性

A total of 22 new heterocyclic hydrazones and their bioisosteric compounds were synthesized and evaluated for their activity against Mycobacterium tuberculosis, strain H37Rv. 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-pyrimi- dimyl)-hydrazone (1d) showed the most effective anti-tubercular activity with MIC₉₀ value of 2 μg/mL, 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/mL, respectively.

Key words: heterocyclic hydrazone analogs, synthesis, Mycobacterium tuberculosis, anti-mycobacterial activity

引用此文

李忠洲, 赵升, 李新军, 王翠翠, 姚璐璐, 金瑞良, 邹新琢. 杂环酮腙与类似物的合成及其对结核杆菌的抑制活性[J]. 有机化学, 2015, 35(6): 1310-1319.

Li Zhongzhou, Zhao Sheng, Li Xinjun, Wang Cuicui, Yao Lulu, Jin Ruiliang, Zou Xinzhuo. Synthesis and Anti-mycobacterial Activities of Heterocyclic Hydrazones and Their Bioisosteric Compounds[J]. Chin. J. Org. Chem., 2015, 35(6): 1310-1319.

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