Synthesis and In Vitro protozoocidal evaluation of novel diazabicyclic tropolone derivatives

被引：10
作者：
Khrizman, Alexander
Slack, Rachel D.
Remsing, Richard C.
Little, Susan
Yardley, Vanessa
Moyna, Guillermo
机构：
[1] Univ Sci Philadelphia, Dept Chem & Biochem, Philadelphia, PA 19104 USA
[2] London Sch Hyg & Trop Med, Dept Infect & Trop Dis, London WC1, England
来源：
ARCHIV DER PHARMAZIE | 2007年 / 340卷 / 11期
关键词：
hydrazynes; parasitoses; protozoocidal activity; synthesis; tropolone derivatives;
D O I：
10.1002/ardp.200700143
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis and in vitro antiparasitic activity of twenty-seven novel diazabicycles based on tropolone ethers is presented. The compounds can be readily prepared by means of a high-yielding hetero Diels -Alder reaction using simple and readily available starting materials. Several of the new diazabicycles have in vitro activities against Trypanosoma cruzi, Leishmania donovani, Trypanosoma brucei rhodesiense, and chloroquine-resistant Plasmodium falciparum that are comparable or superior to those of currently employed protozoocidal agents.
引用
收藏
页码：569 / 576
页数：8
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