Selectively guanidinylated derivatives of neamine. Syntheses and inhibition of anthrax lethal factor protease
Selectively guanidinylated derivatives of neamine. Syntheses and inhibition of anthrax lethal factor protease
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DOI：
10.1016/j.bmcl.2006.07.005
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发表时间：
2006-10-01
影响因子：
2.7
通讯作者：
Tang, Cho
中科院分区：
文献类型：
--
作者：
Jiao, Guan-Sheng;Simo, Ondrej;Tang, Cho
通过邻胺的选择性胍基化，制备了一系列邻胺的单、二、三胍基化衍生物。这些分子代表了一种新的支架作为炭疽致死因子锌金属蛋白酶抑制剂。介绍了这些化合物的合成方法，并分析了它们之间的构效关系。此外，还介绍了这些分子对LF抑制机制的初步发现。(c) 2006 Elsevier Ltd.版权所有。
A series of mono-, di-, and tri-guanidinylated derivatives of neamine were prepared via selective guanidinylation of neamine. These molecules represent a novel scaffold as inhibitors of anthrax lethal factor zinc metalloprotease. Methods for the synthesis of these compounds are described, and structure-activity relationships among the series are analyzed. In addition, initial findings regarding the mechanism of LF inhibition for these molecules are presented. (c) 2006 Elsevier Ltd. All rights reserved.