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

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

Research output: Contribution to journalArticlepeer-review

77 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)2481-2486
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume15
Issue number10
DOIs
StatePublished - May 16 2005

Keywords

  • HCV Polymerase
  • Inhibitors

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