Depeptidization efforts on P3-P′2 α-ketoamide inhibitors of HCVNS3-4A serine protease:: Effect on HCV replicon activity

被引:14
作者
Bogen, SL [1 ]
Ruan, S [1 ]
Liu, R [1 ]
Agrawal, S [1 ]
Pichardo, J [1 ]
Prongay, A [1 ]
Baroudy, B [1 ]
Saksena, AK [1 ]
Girijavallabhan, V [1 ]
Njoroge, FG [1 ]
机构
[1] Schering Plough Corp, Res Inst, Kenilworth, NJ 07033 USA
关键词
D O I
10.1016/j.bmcl.2005.12.013
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Depeptidization efforts of the P-3-P-2 region of P-3 capped alpha-ketoamide inhibitor of HCV NS3 serine protease I are reported. We clearly established that N-methylation of the P-2 nitrogen and modification of the P-2' carboxylic acid terminus were essential for activity in the replicon assay. (C) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1621 / 1627
页数:7
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