Discovery of novel potent HCV NS5B polymerase non-nucleoside inhibitors bearing a fused benzofuran scaffold. Issue 5 (1st March 2018)

• Record Type: Journal Article
• Authors: Zhong, Min; Peng, Eric; Huang, Ningwu; Huang, Qi; Huq, Anja; Lau, Meiyen; Colonno, Richard; Li, Leping
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 28:Issue 5(2018)
• Page Start: 963
• Page End: 968
• Publication Date: 2018-03-01
• Subjects: HCV -- NS5B polymerase -- Non-nucleoside inhibitor -- Fused benzofuran; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2018.01.029
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: This letter describes the discovery of a fused benzofuran scaffold viable for preparing a series of novel potent HCV NS5B polymerase non-nucleoside inhibitors. Designed on the basis of the functionalized benzofuran derivative nesbuvir (HCV-796 ), these compounds presumably bind similarly to the allosteric binding site in the "palm" domain of HCV NS5B protein. SAR of each potential hydrogen-bonding interaction site of this novel scaffold is discussed along with some preliminary genotypic profile and PK data of several advanced compounds.