P2-P4 macrocyclic inhibitors of hepatitis C virus NS3-4A serine protease

Ashok Arasappan; F George Njoroge; Kevin X Chen; Srikanth Venkatraman; Tejal N Parekh; Haining Gu; John Pichardo; Nancy Butkiewicz; Andrew Prongay; Vincent Madison; Viyyoor Girijavallabhan

doi:10.1016/j.bmcl.2006.05.022

P2-P4 macrocyclic inhibitors of hepatitis C virus NS3-4A serine protease

Bioorg Med Chem Lett. 2006 Aug 1;16(15):3960-5. doi: 10.1016/j.bmcl.2006.05.022. Epub 2006 May 30.

Authors

Ashok Arasappan¹, F George Njoroge, Kevin X Chen, Srikanth Venkatraman, Tejal N Parekh, Haining Gu, John Pichardo, Nancy Butkiewicz, Andrew Prongay, Vincent Madison, Viyyoor Girijavallabhan

Affiliation

¹ Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. [email protected]

PMID: 16730985
DOI: 10.1016/j.bmcl.2006.05.022

Abstract

Synthesis and HCV NS3 serine protease inhibitory activity of 4-hydroxyproline derived macrocyclic inhibitors and SAR around this macrocyclic core is described in this communication. X-ray structure of inhibitor 38 bound to the protease is discussed.

MeSH terms

Hepatitis C / enzymology*
Macrocyclic Compounds / pharmacology*
Serine Proteinase Inhibitors / pharmacology*
Viral Nonstructural Proteins / antagonists & inhibitors*
X-Ray Diffraction

Substances

Macrocyclic Compounds
NS3 protein, hepatitis C virus
Serine Proteinase Inhibitors
Viral Nonstructural Proteins