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

doi:10.1016/j.bmcl.2005.03.066

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

Medicinal Chemistry

Research output: Contribution to journal › Article › peer-review

84 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 language	English (US)
Pages (from-to)	2481-2486
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	15
Issue number	10
DOIs	https://doi.org/10.1016/j.bmcl.2005.03.066
State	Published - May 16 2005

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

HCV Polymerase
Inhibitors

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10.1016/j.bmcl.2005.03.066

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Pfefferkorn, J. A., Greene, M. L., Nugent, R. A., Gross, R. J., Mitchell, M. A., Finzel, B. C., Harris, M. S., Wells, P. A., Shelly, J. A., Anstadt, R. A., Kilkuskie, R. E., Kopta, L. A., & Schwende, F. J. (2005). Inhibitors of HCV NS5B polymerase. Part 1: Evaluation of the southern region of (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid. Bioorganic and Medicinal Chemistry Letters, 15(10), 2481-2486. https://doi.org/10.1016/j.bmcl.2005.03.066

Pfefferkorn, JA, Greene, ML, Nugent, RA, Gross, RJ, Mitchell, MA, Finzel, BC, Harris, MS, Wells, PA, Shelly, JA, Anstadt, RA, Kilkuskie, RE, Kopta, LA & Schwende, FJ 2005, 'Inhibitors of HCV NS5B polymerase. Part 1: Evaluation of the southern region of (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid', Bioorganic and Medicinal Chemistry Letters, vol. 15, no. 10, pp. 2481-2486. https://doi.org/10.1016/j.bmcl.2005.03.066

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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.",

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

Abstract

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