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ID: ALA1135083
Journal: Bioorg Med Chem Lett
Title: A designed P1 cysteine mimetic for covalent and non-covalent inhibitors of HCV NS3 protease.
Authors: Narjes F, Koehler KF, Koch U, Gerlach B, Colarusso S, Steinkühler C, Brunetti M, Altamura S, De Francesco R, Matassa VG.
Abstract: The difluoromethyl group was designed by computational chemistry methods as a mimetic of the canonical P1 cysteine thiol for inhibitors of the hepatitis C virus NS3 protease. This modification led to the development of competitive, non-covalent inhibitor 4 (K(i) 30 nM) and reversible covalent inhibitors (6, K(i) 0.5 nM; and 8 K*(i) 10 pM).
CiteXplore: 11844705