Structural highlights
Evolutionary Conservation
Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.
Publication Abstract from PubMed
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.
Inhibitors of HCV NS5B polymerase. Part 1: Evaluation of the southern region of (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid.,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 Bioorg Med Chem Lett. 2005 May 16;15(10):2481-6. PMID:15863301[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ 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. Inhibitors of HCV NS5B polymerase. Part 1: Evaluation of the southern region of (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid. Bioorg Med Chem Lett. 2005 May 16;15(10):2481-6. PMID:15863301 doi:10.1016/j.bmcl.2005.03.066