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源自依他尼酸的恶性疟原虫非肽类半胱氨酸蛋白酶抑制剂的合成与评价

Synthesis and evaluation of non-peptidic cysteine protease inhibitors of P. falciparum derived from etacrynic acid.

作者信息

Dude Marie-Adrienne, Kaeppler Ulrich, Herb Monika, Schiller Markus, Schulz Franziska, Vedder Birgit, Heppner Saskia, Pradel Gabriele, Gut Jiri, Rosenthal Philip J, Schirmeister Tanja, Leippe Matthias, Gelhaus Christoph

机构信息

Research Center for Infectious Diseases, University of Würzburg, Röntgenring 11, 97070 Würzburg, Germany.

出版信息

Molecules. 2008 Dec 23;14(1):19-35. doi: 10.3390/molecules14010019.

DOI:10.3390/molecules14010019
PMID:19104483
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6253875/
Abstract

A series of etacrynic acid derivatives was synthesized and screened for their in vitro activity against Plasmodium falciparum, as well as their activity against recombinantly expressed falcipain-2 and -3. The two most active compounds of the series displayed IC(50) values of 9.0 and 18.8 microM against Plasmodia.

摘要

合成了一系列依他尼酸衍生物，并对其抗恶性疟原虫的体外活性以及对重组表达的疟原虫蛋白酶-2和-3的活性进行了筛选。该系列中活性最高的两种化合物对疟原虫的半数抑制浓度（IC50）值分别为9.0和18.8微摩尔。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4bf/6253875/a46a5fc51dcf/molecules-14-00019-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4bf/6253875/9e06c1b70bc9/molecules-14-00019-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4bf/6253875/a46a5fc51dcf/molecules-14-00019-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4bf/6253875/9e06c1b70bc9/molecules-14-00019-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4bf/6253875/a46a5fc51dcf/molecules-14-00019-g002.jpg

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本文引用的文献

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Imidazolidin-4-one peptidomimetic derivatives of primaquine: synthesis and antimalarial activity.伯氨喹的咪唑烷-4-酮肽模拟物衍生物：合成与抗疟活性
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Development of peptidomimetics with a vinyl sulfone warhead as irreversible falcipain-2 inhibitors.具有乙烯砜弹头的拟肽作为不可逆的恶性疟原虫裂殖子蛋白酶-2抑制剂的开发。
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