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

被引：0
|
作者：
Li, Zhongzhou [1 ]
Zhao, Sheng [1 ]
Li, Xinjun [1 ]
Wang, Cuicui [1 ]
Yao, Lulu [1 ]
Jin, Ruiliang [2 ]
Zou, Xinzhou [1 ]
机构：
[1] E China Normal Univ, Dept Chem, Shanghai 200241, Peoples R China
[2] Tongji Univ, Shanghai Key Lab TB, Shanghai Pulm Hosp, Shanghai 200433, Peoples R China
来源：
CHINESE JOURNAL OF ORGANIC CHEMISTRY | 2015年 / 35卷 / 06期
关键词：
heterocyclic hydrazone analogs; synthesis; Mycobacterium tuberculosis; anti-mycobacterial activity; ANALOGS; MYCOBACTERIA; CURCUMIN; DESIGN; SERIES;
D O I：
10.6023/cjoc201412011
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
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-pyrimidimyl)-hydrazone (1d) showed the most effective anti-tubercular activity with MIC90 value of 2 mu g/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 mu g/mL, respectively.
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页码：1310 / 1319
页数：10
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