新型2-氧代咪唑烷-4-羧酸衍生物作为丙型肝炎病毒NS3-4A丝氨酸蛋白酶抑制剂：酶抑制剂复合物的合成、活性及X射线晶体结构
Novel 2-oxoimidazolidine-4-carboxylic acid derivatives as hepatitis C virus NS3-4A serine protease inhibitors: synthesis, activity, and X-ray crystal structure of an enzyme inhibitor complex.
作者信息
Arasappan Ashok, Njoroge F George, Parekh Tejal N, Yang Xiaozheng, Pichardo John, Butkiewicz Nancy, Prongay Andrew, Yao Nanhua, Girijavallabhan Viyyoor
机构信息
Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
出版信息
Bioorg Med Chem Lett. 2004 Dec 6;14(23):5751-5. doi: 10.1016/j.bmcl.2004.09.058.
PMID:15501035
Abstract
Synthesis and HCV NS3 serine protease inhibitory activity of some novel 2-oxoimidazolidine-4-carboxylic acid derivatives are reported. Inhibitors derived from this new P2 core exhibited activity in the low microM range. X-ray structure of an inhibitor, 15c bound to the protease is presented.
摘要
报道了一些新型2-氧代咪唑烷-4-羧酸衍生物的合成及其对丙型肝炎病毒NS3丝氨酸蛋白酶的抑制活性。源自这种新的P2核心的抑制剂在低微摩尔范围内表现出活性。给出了与蛋白酶结合的抑制剂15c的X射线结构。
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