Chinese Journal of Organic Chemistry >
Synthesis and Anti-mycobacterial Activities of Heterocyclic Hydrazones and Their Bioisosteric Compounds
Received date: 2014-12-04
Revised date: 2015-01-21
Online published: 2015-02-02
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.
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]. Chinese Journal of Organic Chemistry, 2015 , 35(6) : 1310 -1319 . DOI: 10.6023/cjoc201412011
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