Discovery of a potent and selective noncovalent linear inhibitor of the hepatitis C virus NS3 protease (BI 201335)

M Llinas-Brunet, MD Bailey, N Goudreau…

文献索引：Llinas-Brunet, Montse; Bailey, Murray D.; Ghiro, Elise; Gorys, Vida; Halmos, Ted; Poirier, Martin; Rancourt, Jean; Goudreau, Nathalie Journal of Medicinal Chemistry, 2004 , vol. 47, # 26 p. 6584 - 6594

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被引用次数: 67

摘要

C-Terminal carboxylic acid containing inhibitors of the NS3 protease are reported. A novel series of linear tripeptide inhibitors that are very potent and selective against the NS3 protease are described. A substantial contribution to the potency of these linear inhibitors arises from the introduction of a C8 substituent on the B-ring of the quinoline moiety found on the P2 of these inhibitors. The introduction of a C8 methyl group results not only in a ...