Novel tripeptide inhibitors of hepatitis C virus NS3 serine protease

Abstract

Available therapies for hepatitis C viral infection, a disease with a growing impact worldwide, have limited success and serious side effects. Among different possibilities to control the infection, the NS3 serine protease inhibitors constitute a promising alternative, based on a similar approach proved successful in the case of HIV antiviral agents. However, the structural particularities of this viral serine protease make the design of small molecule inhibitors a difficult task. In contrast, the peptidic and peptidomimetic approach gave better results, allowing submicromolar levels of inhibition. In this patent, Bristol-Myers Squibb presents new tripeptide inhibitors with improved potency against NS3 protease and a very good selectivity against related serine proteases. The disclosed compounds also exhibited a good inhibitory profile against different viral strain proteases, giving good hopes to the use of NS3 protease inhibitors as a cure to treat hepatitis C viral infections.

• antiviral agents
• hepatitis C virus (HCV)
• NS3 serine protease
• tripeptide inhibitors