Bismacrocyclic Inhibitors of Hepatitis C NS3/4a Protease

被引：32

作者：

McCauley, John A. ^{[1
]}

Rudd, Michael T. ^{[1
]}

Nguyen, Kevin T. ^{[1
]}

McIntyre, Charles J. ^{[1
]}

Romano, Joseph J. ^{[1
]}

Bush, Kimberly J. ^{[1
]}

Varga, Sandor L. ^{[1
]}

Ross, Charles W., III ^{[1
]}

Carroll, Steven S. ^{[2
]}

DiMuzio, Jillian ^{[2
]}

Stahlhut, Mark W. ^{[2
]}

Olsen, David B. ^{[2
]}

Lyle, Terry A. ^{[1
]}

Vacca, Joseph P. ^{[1
]}

Liverton, Nigel J. ^{[1
]}

机构：

[1] Merck Res Labs, Dept Med Chem, West Point, PA 19486 USA

[2] Merck Res Labs, Dept Antiviral Res, West Point, PA USA

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2008年 / 47卷 / 47期

关键词：

hepatitis C; inhibitors; macrocycles; ring-closing metathesis; ruthenium;

D O I：

10.1002/anie.200803298

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

(Chemical Equation Presented) Double time: The bismacrocycle 2 was prepared from 1 by a selective double ring-closing metathesis (RCM) reaction to form the 18- and 15-membered rings simultaneously. Derivative 3 shows excellent potency against NS3/4a protease. © 2008 Wiley-VCH Verlag GmbH & Co. KGaA.

引用

页码：9104 / 9107

页数：4

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