909400-45-9Relevant academic research and scientific papers
Novel peptide mimetics based on N-Protected amino acids derived from isomannide as potential inhibitors of NS3 serine protease of hepatitis C virus
Barros, Thalita G.,Zorzanelli, Bruna C.,Pinheiro, Sergio,De Brito, Monique A.,Tanuri, Amilcar,Da Costa, Emmerson C.B.,Mohana-Borges, Ronaldo S.,Rodrigues, Carlos R.,Souza, Alessandra T.M.,Ferreira, Vitor F.,Muri, Estela M.F.
, p. 239 - 249 (2012/07/27)
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.
Novel peptide mimetic inhibitors of hepatitis C serine protease derived from isomannide
Barros, Thalita G.,Pinheiro, Sergio,Williamson, John S.,Tanuri, Amilcar,Pereira, Helena S.,Brindeiro, Rodrigo M.,Neto, Jose B. A.,Antunes, Octavio A. C.,Muri, Estela M. F.
experimental part, p. 620 - 626 (2009/06/28)
Hepatitis C (HCV) infection is a cause of chronic liver disease such as cirrhosis, carcinoma, or liver failure, and the current therapy is effective in only 50% of patients. Serine proteases, which are present in HCV, are the most studied class of proteolytic enzymes, and are a primary target in the drug development field. In this paper, we describe the synthesis and biological studies of a novel class of peptide mimetic compounds as potential HCV serine protease inhibitors. Georg Thieme Verlag Stuttgart.
