Phenethyl amides as novel noncovalent inhibitors of hepatitis C virus NS3/4A protease: Discovery, initial SAR, and molecular modeling
The discovery of novel, reversible and competitive tripeptide inhibitors of the Hepatitis C virus NS3/4A serine protease is described. These inhibitors are characterized by the presence of a C-terminal phenethyl amide group, which extends into the prime side of the enzyme. Initial SAR together with molecular modeling and data from site-directed mutagenesis suggest an interaction of the phenethyl amide group with Lys-136.
Colarusso, Stefania,Koch, Uwe,Gerlach, Benjamin,Steinkühler, Christian,De Francesco, Raffaele,Altamura, Sergio,Matassa, Victor G.,Narjes, Frank
p. 345 - 348
(2007/10/03)
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