Synthesis and evaluation of phenoxyoxazaphospholidine, phenoxyoxazaphosphinane, and benzodioxaphosphininamine sulfides and related compounds as potential anti-malarial agents

被引：6

作者：

Mara, Christine ^{[1
]}

Dempsey, Enda ^{[2
]}

Bell, Angus ^{[2
]}

Barlow, James W. ^{[1
]}

机构：

[1] Royal Coll Surgeons Ireland, Dept Pharmaceut & Med Chem, Dublin 2, Ireland

[2] Trinity Coll Dublin, Moyne Inst Prevent Med, Sch Genet & Microbiol, Dept Microbiol, Dublin 2, Ireland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 12期

关键词：

Phenoxyoxazaphospholidines; Phenoxyoxazaphosphinanes; Benzodioxaphosphininamines; Anti-malarial; Tubulin; DRUG DISCOVERY;

D O I：

10.1016/j.bmcl.2013.04.026

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of phenoxyoxazaphospholidine, phenoxyoxazaphosphinane and benzodioxaphosphininamine sulfides and related cyclic organophosphorus compounds based on the lead anti-tubulin herbicides amiprophos methyl and butamifos were synthesised and evaluated for anti-malarial activity. Of these compounds, while none of the phenoxyoxazaphospholidines, phenoxyoxazaphosphinanes or benzodioxaphosphininamine sulphides were more potent than APM, phosphorothioamidate 30, a dual compound also bearing an aminoquinoline motif, showed promising activity against Plasmodium falciparum (IC50 0.038 mu M) and warrants further study. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：3580 / 3583

页数：4

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