Portal de Periódicos da CAPES

Inhibitors of HCV NS5B polymerase. Part 1: Evaluation of the southern region of (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid

2005; Elsevier BV; Volume: 15; Issue: 10 Linguagem: Inglês

10.1016/j.bmcl.2005.03.066

1464-3405

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

Biochemical and Molecular Research

A novel series of nonnucleoside HCV NS5B polymerase inhibitors were prepared from (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid, a high throughput screening lead. SAR studies combined with structure based drug design focusing on the southern heterobiaryl region of the template led to the synthesis of several potent and orally bioavailable lead compounds. X-ray crystallography studies were also performed to understand the interaction of these inhibitors with HCV NS5B polymerase.