SAR and pharmacokinetic studies on phenethylamide inhibitors of the hepatitis C virus NS3/NS4A serine protease

被引:22
作者
Malancona, S
Colarusso, S
Ontoria, JM
Marchetti, A
Poma, M
Stansfield, I
Laufer, R
Di Marco, A
Taliani, M
Verdirame, M
Gonzalez-Paz, O
Matassa, VG
Narjes, F
机构
[1] Merck Res Labs, Dept Chem, Ist Ric Biol Mol P Angeletti, I-00040 Rome, Italy
[2] Merck Res Labs, Dept Pharmacol, Ist Ric Biol Mol P Angeletti, I-00040 Rome, Italy
关键词
D O I
10.1016/j.bmcl.2004.05.093
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
SAR on the phenethylamide I (K-i 1.2 muM) in the P2- and the V-position led to potent inhibitors, one of which showed good exposure and low clearance when administered intramuscularly to rat. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4575 / 4579
页数:5
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