Phosphonium lipocations as antiparasitic agents

被引:24
作者
Long, Timothy E. [1 ,2 ]
Lu, Xiao [1 ,2 ]
Galizzi, Melina [3 ,4 ]
Docampo, Roberto [3 ,4 ]
Gut, Jiri [5 ]
Rosenthal, Philip J. [5 ]
机构
[1] Univ Georgia, Dept Pharmaceut & Biomed Sci, Athens, GA 30602 USA
[2] Univ Georgia, Ctr Drug Discovery, Athens, GA 30602 USA
[3] Univ Georgia, Ctr Trop & Emerging Global Dis, Athens, GA 30602 USA
[4] Univ Georgia, Dept Cellular Biol, Athens, GA 30602 USA
[5] Univ Calif San Francisco, Dept Med, San Francisco Gen Hosp, San Francisco, CA 94143 USA
基金
美国国家卫生研究院;
关键词
Malaria; Chagas; Antiparasitic drugs; Plasmodium; Trypanosoma; VISIBLE LIPIDS; MITOCHONDRIA; SALTS; CATIONS; DRUGS; CHEMOTHERAPY; ANTIOXIDANT; ARTEMISININ; INHIBITION; ACTIVATION;
D O I
10.1016/j.bmcl.2012.02.045
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Phosphonium lipocations were synthesized and evaluated for inhibition of the development of Plasmodium falciparum and Trypanosoma cruzi, etiological agents of malaria and Chagas disease, respectively. Optimal phthalimides and 1,4-naphthoquinone-based lipocations were active in vitro at mid-high nM concentrations against P. falciparum and low mu M concentrations against T. cruzi. Published by Elsevier Ltd.
引用
收藏
页码:2976 / 2979
页数:4
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