Hepatitis C virus (HCV) is among the most important flaviviruses. It has a serine protease which is important for viral replication and this enzyme constitutes a suitable target for new anti-retroviral drugs. Herein we disclose a series of amide and ester peptide mimetic inhibitors of serine proteases, all of them obtained via coupling reactions of isomannide derivatives with N-protected amino acids. The arginine derivative 19 showed 45% of inhibition of NS3/4A serine protease at 100 μM and molecular modeling studies had shown that 19 interacted with the active site of this enzyme.
Keywords: HCV, isomannide, peptide mimetic, serine protease, hepatocellular carcinoma, structural manipulation, bioavailability, administration, dipeptides, scaffold
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Published on: 24 April, 2012
Page: [239 - 249]