Design and synthesis of potent, non-peptide inhibitors of HCV NS3 protease

Xiaojun Zhang; Aaron C Schmitt; Wen Jiang; Zelda Wasserman; Carl P Decicco

doi:10.1016/s0960-894x(03)00032-5

Design and synthesis of potent, non-peptide inhibitors of HCV NS3 protease

Bioorg Med Chem Lett. 2003 Mar 24;13(6):1157-60. doi: 10.1016/s0960-894x(03)00032-5.

Authors

Xiaojun Zhang¹, Aaron C Schmitt, Wen Jiang, Zelda Wasserman, Carl P Decicco

Affiliation

¹ Discovery Chemistry, Bristol-Myers Squibb, Route 141 and Henry Clay Road, Wilmington, DE 19880, USA. xiaojun.zhang@bms.com

PMID: 12643933
DOI: 10.1016/s0960-894x(03)00032-5

Abstract

Starting from a hexapeptide boronic acid lead, 3-amino bicyclic pyrazinones as novel beta-sheet dipeptide mimetics have been designed and synthesized. Side-chain manipulation of this scaffold generated a series of potent, nonpeptidic inhibitors of HCV NS3 protease.

MeSH terms

Crystallography, X-Ray
Hepacivirus / drug effects
Hepacivirus / enzymology*
Models, Molecular
Protease Inhibitors / chemical synthesis*
Protease Inhibitors / pharmacology*
Protein Conformation
Structure-Activity Relationship
Viral Nonstructural Proteins / chemistry*

Substances

NS3 protein, hepatitis C virus
Protease Inhibitors
Viral Nonstructural Proteins