Synthesis and bio-evaluation of phenothiazine derivatives as new antituberculosis agents

注册 English

Synthesis and bio-evaluation of phenothiazine derivatives as new antituberculosis agents

Chun-Xian He , Hui Meng , Xiang Zhang , Hua-Qing Cui , Da-Li Yin

Citation: Chun-Xian He, Hui Meng, Xiang Zhang, Hua-Qing Cui, Da-Li Yin. Synthesis and bio-evaluation of phenothiazine derivatives as new antituberculosis agents[J]. Chinese Chemical Letters, 2015, 26(8): 951-954. doi: 10.1016/j.cclet.2015.03.027 shu

shu

Synthesis and bio-evaluation of phenothiazine derivatives as new antituberculosis agents

Chun-Xian He ^a, ,
Hui Meng ^b, ,
Xiang Zhang ^a, ,
Hua-Qing Cui ^{c,
,} ,
Da-Li Yin ^{a,
,}

通讯作者: Hua-Qing Cui,
Da-Li Yin,

基金项目:

Development Program ("863"Program) of China" (No. 2012AA020302) for financial support. ("863"Program)

摘要: Two series of phenothiazine derivatives were designed and synthesized. All compounds were tested for anti-tuberculosis activities against Mycobacterium tuberculosis H₃₇R_V. In comparison with mother compound of chlorpromazine, compound 6e shows promising anti-tuberculosis activity and much less mammalian cell cytotoxicity, compound 6e merits to be further explored as new anti-tuberculosis agents.

关键词:

English

Synthesis and bio-evaluation of phenothiazine derivatives as new antituberculosis agents

Chun-Xian He ^a, ,
Hui Meng ^b, ,
Xiang Zhang ^a, ,
Hua-Qing Cui ^{c,
,} ,
Da-Li Yin ^{a,
,}

1.
a State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China;
2.
b College of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan 250355, China;
3.
c Department of Medicinal Chemistry, Beijing Key Laboratory of Active Substances Discovery and Drugability Evaluation, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China

Corresponding author: Hua-Qing Cui, Da-Li Yin,

Received Date: 01 December 2014
Available Online: 28 March 2015

Abstract: Two series of phenothiazine derivatives were designed and synthesized. All compounds were tested for anti-tuberculosis activities against Mycobacterium tuberculosis H₃₇R_V. In comparison with mother compound of chlorpromazine, compound 6e shows promising anti-tuberculosis activity and much less mammalian cell cytotoxicity, compound 6e merits to be further explored as new anti-tuberculosis agents.

Key words:

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