丙型肝炎病毒NS3蛋白酶的强效抑制剂：一种新型P2环戊烷衍生模板的应用
Potent inhibitors of the hepatitis C virus NS3 protease: use of a novel P2 cyclopentane-derived template.
作者信息
Johansson Per-Ola, Bäck Marcus, Kvarnström Ingemar, Jansson Katarina, Vrang Lotta, Hamelink Elizabeth, Hallberg Anders, Rosenquist Asa, Samuelsson Bertil
机构信息
Department of Chemistry, Linköping University, S-581 83 Linköping, Sweden.
出版信息
Bioorg Med Chem. 2006 Aug 1;14(15):5136-51. doi: 10.1016/j.bmc.2006.04.008. Epub 2006 May 3.
The HCV NS3 protease is essential for replication of the hepatitis C virus (HCV) and therefore constitutes a promising new drug target for anti-HCV therapy. Several potent and promising HCV NS3 protease inhibitors, some of which display low nanomolar activities, were identified from a series of novel inhibitors incorporating a trisubstituted cyclopentane dicarboxylic acid moiety as a surrogate for the widely used N-acyl-(4R)-hydroxyproline in the P2 position.
丙型肝炎病毒（HCV）NS3蛋白酶对于丙型肝炎病毒的复制至关重要，因此是抗HCV治疗中一个很有前景的新药物靶点。从一系列新型抑制剂中鉴定出了几种强效且有前景的HCV NS3蛋白酶抑制剂，其中一些表现出低纳摩尔活性，这些抑制剂含有三取代环戊烷二羧酸部分，作为P2位广泛使用的N-酰基-（4R）-羟基脯氨酸的替代物。
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