Hepatitis C virus NS3-4A serine protease inhibitors:: SAR of P′2 moiety with improved potency

被引：26

作者：

Arasappan, A

Njoroge, FG

Chan, TY

Bennett, F

Bogen, SL

Chen, K

Gu, H

Hong, L

Jao, E

Liu, YT

Lovey, RG

Parekh, T

Pike, RE

Pinto, P

Santhanam, B

Venkatraman, S

Vaccaro, H

Wang, H

Yang, X

Zhu, Z

Mckittrick, B

Saksena, AK

Girijavallabhan, V

Pichardo, J

Butkiewicz, N

Ingram, R

Malcolm, B

Prongay, A

Yao, N

Marten, B

Madison, V

Kemp, S

Levy, O

Lim-Wilby, M

Tamura, S

Gangulya, AK

机构：

[1] Schering Plough Res Inst, Kenilworth, NJ 07033 USA

[2] Dendreon Corp, Seattle, WA 98121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 19期

关键词：

D O I：

10.1016/j.bmcl.2005.06.091

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have discovered that introduction of appropriate amino acid derivatives at P-2(') position improved the binding potency of P-3-capped alpha-ketoamide inhibitors of HCV NS3 serine protease. X-ray crystal structure of one of the inhibitors (43) bound to the protease revealed the importance of the P-2(') moiety. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：4180 / 4184

页数：5

共 23 条

[11] READILY ACCESSIBLE 12-I-5 OXIDANT FOR THE CONVERSION OF PRIMARY AND SECONDARY ALCOHOLS TO ALDEHYDES AND KETONES [J].