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

页码：72 / 76

页数：5

共 32 条

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