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Inhibitors of HCV NS5B polymerase. Part 2: Evaluation of the northern region of (2Z)-2-benzoylamino-3-(4-phenoxy-phenyl)-acrylic acid

2005; Elsevier BV; Volume: 15; Issue: 11 Linguagem: Inglês

10.1016/j.bmcl.2005.03.106

1464-3405

Jeffrey A. Pfefferkorn, Richard A. Nugent, Rebecca J. Gross, Meredith Greene, Mark A. Mitchell, Matthew T. Reding, Lee Funk, Rebecca M. Anderson, Peter A. Wells, John A. Shelly, Robert A. Anstadt, B.C. Finzel, Melissa S. Harris, Robert E. Kilkuskie, Laurice A. Kopta, Francis J. Schwende,

Monoclonal and Polyclonal Antibodies Research

A novel series of non-nucleoside HCV NS5B polymerase inhibitors was prepared from a (2Z)-2-benzoylamino-3-(4-phenoxy-phenyl)-acrylic acid template. Solution and solid phase analog synthesis focused on the northern region of the template combined with structure based design led to the discovery of several potent and orally bioavailable lead compounds.