Design, Synthesis, and Antiplasmodial Activity of Hybrid Compounds Based on (2R,3S)-N-Benzoyl-3-phenylisoserine

被引：30
|
作者：
Njogu, Peter M. [1 ]
Gut, Jiri [2 ]
Rosenthal, Philip J. [2 ]
Chibale, Kelly [1 ,3 ]
机构：
[1] Univ Cape Town, Dept Chem, ZA-7701 Rondebosch, South Africa
[2] Univ Calif San Francisco, San Francisco Gen Hosp, Dept Med, San Francisco, CA 94143 USA
[3] Univ Cape Town, Inst Infect Dis & Mol Med, ZA-7701 Rondebosch, South Africa
来源：
ACS MEDICINAL CHEMISTRY LETTERS | 2013年 / 4卷 / 07期
基金：
新加坡国家研究基金会; 英国医学研究理事会;
关键词：
(2R; 3S)-N-Benzoyl-3-phenylisoserine; artemisinin; quinoline; hybrids; antiplasmodial activity; DRUG DISCOVERY; MALARIA; AGENTS; TAXOL;
D O I：
10.1021/ml400164t
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of hybrid compounds based, on.(2R,3S)-N-benzoyl-3-phenylisoserine, artemisinin, and quinoline moieties was synthesized and tested for in vitro antiplasmodial activity against erythrocytic stages of K1 and W2 strains of Plasmodium falciparum Two hybrid compounds incorporating (2R,3S)-N-benzoyl-3-phenylisoserine and artemisinin scaffolds were 3- to 4-fold more active than dihydroartemisinin, with nanomolar IC50 values against Plasmodium falciparum K1 strain.
引用
收藏
页码：72 / 76
页数：5
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