Phosphonium lipocations as antiparasitic agents

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:22

Article

Long, Timothy E.^1,2  Lu, Xiao^1,2  Galizzi, Melina^3,4  Docampo, Roberto^3,4  Gut, Jiri⁵  Rosenthal, Philip J.⁵ 

[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

关键词: Malaria;    Chagas;    Antiparasitic drugs;    Plasmodium;    Trypanosoma;   

DOI  :  10.1016/j.bmcl.2012.02.045

来源: Elsevier

【 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.

【 授权许可】

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