Johansson Per-Ola, Bäck Marcus, Kvarnström Ingemar, Jansson Katarina, Vrang Lotta, Hamelink Elizabeth, Hallberg Anders, Rosenquist Asa, Samuelsson Bertil
Department of Chemistry, Linköping University, S-581 83 Linköping, Sweden.
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。
