Synthesis and antiviral activity of novel HCV NS3 protease inhibitors with P4 capping groups.
Basic Information
ID: ALA2202978
Journal: Bioorg Med Chem Lett
Title: Synthesis and antiviral activity of novel HCV NS3 protease inhibitors with P4 capping groups.
Authors: Li X, Liu Y, Zhang YK, Plattner JJ, Baker SJ, Bu W, Liu L, Zhou Y, Ding CZ, Zhang S, Kazmierski WM, Hamatake R, Duan M, Wright LL, Smith GK, Jarvest RL, Ji JJ, Cooper JP, Tallant MD, Crosby RM, Creech K, Wang A.
Abstract: We have synthesized and evaluated a series of novel HCV NS3 protease inhibitors with various P4 capping groups, which include urea, carbamate, methoxy-carboxamide, cyclic carbamate and amide, pyruvic amide, oxamate, oxalamide and cyanoguanidine. Most of these compounds are remarkably potent, exhibiting single-digit to sub-nanomolar activity in the enzyme assay and cell-based replicon assay. Selected compounds were also evaluated in the protease-inhibitor-resistant mutant transient replicon assay, and they were found to show quite different potency profiles against a panel of HCV protease-inhibitor-resistant mutants.
CiteXplore: 23142614
DOI: 10.1016/j.bmcl.2012.10.075
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