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磷霉素和FR900098的链取代新戊酰氧基甲酯类似物的合成及其抗疟活性

Synthesis and antimalarial activity of chain substituted pivaloyloxymethyl ester analogues of Fosmidomycin and FR900098.

作者信息

Kurz Thomas, Schlüter Katrin, Kaula Uwe, Bergmann Bärbel, Walter Rolf D, Geffken Detlef

机构信息

Institute of Pharmacy, University of Hamburg, Bundesstrasse 45, D-20146 Hamburg, Germany.

出版信息

Bioorg Med Chem. 2006 Aug 1;14(15):5121-35. doi: 10.1016/j.bmc.2006.04.018. Epub 2006 May 5.

DOI:10.1016/j.bmc.2006.04.018
PMID:16679022
Abstract

Fosmidomycin is a promising antimalarial drug candidate with a unique chemical structure and a novel mode of action. Chain substituted pivaloyloxymethyl ester derivatives of Fosmidomycin and its acetyl analogue FR900098 have been synthesized and their in vitro antimalarial activity versus the Chloroquine sensitive strain 3D7 of Plasmodium falciparum has been determined.

摘要

磷霉素是一种有前景的抗疟药物候选物,具有独特的化学结构和新颖的作用模式。已合成了磷霉素的链取代新戊酰氧基甲酯衍生物及其乙酰类似物FR900098,并测定了它们对恶性疟原虫氯喹敏感株3D7的体外抗疟活性。

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Synthesis and antimalarial activity of chain substituted pivaloyloxymethyl ester analogues of Fosmidomycin and FR900098.磷霉素和FR900098的链取代新戊酰氧基甲酯类似物的合成及其抗疟活性
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