诺如病毒 3C 蛋白酶抑制剂的设计、合成与评价。
Design, synthesis, and evaluation of inhibitors of Norwalk virus 3C protease.
机构信息
Department of Chemistry, Wichita State University, Wichita, KS 67260, USA.
出版信息
Bioorg Med Chem Lett. 2011 Sep 15;21(18):5315-9. doi: 10.1016/j.bmcl.2011.07.016. Epub 2011 Jul 14.
Abstract
The first series of peptidyl aldehyde inhibitors that incorporate in their structure a glutamine surrogate has been designed and synthesized based on the known substrate specificity of Norwalk virus 3C protease. The inhibitory activity of the compounds with the protease and with a norovirus cell-based replicon system was investigated. Members of this class of compounds exhibited noteworthy activity both in vitro and in a cell-based replicon system.
摘要
基于诺如病毒 3C 蛋白酶已知的底物特异性，我们设计并合成了第一个包含谷氨酰胺类似物结构的肽酰醛抑制剂系列。我们研究了这些化合物与蛋白酶以及诺如病毒基于细胞的复制子系统的抑制活性。该类化合物在体外和基于细胞的复制子系统中均表现出显著的活性。
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