丙型肝炎病毒NS3蛋白酶的封端二肽苯乙酰胺抑制剂。
Capped dipeptide phenethylamide inhibitors of the HCV NS3 protease.
作者信息
Nizi Emanuela, Koch Uwe, Ontoria Jesus M, Marchetti Antonella, Narjes Frank, Malancona Savina, Matassa Victor G, Gardelli Cristina
机构信息
Department of Chemistry, IRBM, MRL Rome, Via Pontina Km 30,600, 00040 Pomezia, Rome, Italy.
出版信息
Bioorg Med Chem Lett. 2004 May 3;14(9):2151-4. doi: 10.1016/j.bmcl.2004.02.032.
PMID:15080998
Abstract
The N-terminal aminoacid of phenethylamide tripeptide inhibitors of the hepatitis C virus NS3 protease can be replaced with an alpha-hydroxy acid to obtain more 'drug like' inhibitors with low micromolar activity. The preferred S-configuration of the capping residue can be explained by molecular modeling studies.
摘要
丙型肝炎病毒NS3蛋白酶的苯乙酰胺三肽抑制剂的N端氨基酸可用α-羟基酸替代，以获得具有低微摩尔活性的更具“药物样”的抑制剂。封端残基的优选S构型可通过分子模拟研究来解释。
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