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Novel Peptide Mimetics Based on N-protected Amino Acids Derived from Isomannide as Potential Inhibitors of NS3 Serine Protease of Hepatitis C Virus

[ Vol. 9 , Issue. 4 ]

Author(s):

Thalita G. Barros, Bruna C. Zorzanelli, Sergio Pinheiro, Monique A. de Brito, Amilcar Tanuri, Emmerson C.B. da Costa, Ronaldo S. Mohana-Borges, Carlos R. Rodrigues, Alessandra T.M. Souza, Vitor F. Ferreira and Estela M.F. Muri   Pages 239 - 249 ( 11 )

Abstract:


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

Affiliation:

Departamento de Tecnologia Farmaceutica/MTC Faculdade de Farmacia Universidade Federal Fluminense– UFF Rua Mario Viana 523, Santa Rosa/Niteroi/RJ; Cep: 24241-000.



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