In this presentation, we describe the synthesis and SAR of a series of acyclic triazines which function as entry inhibitors of the hepatitis C virus.  An early lead in this series, 4-(4-(1-(4-chlorophenyl)cyclopropylamino)-6-(2,2,2-trifluoroethoxy)-1,3,5-triazin-2-ylamino)benzoic acid, served as the starting point for optimization. These SAR studies led to the identification of an acylsulfonamide series in which the acylsulfonamide moiety serves as a replacement for the carboxylic acid present in the early lead.  A number of compounds from this chemotype displayed enhanced inhibitory activity toward genotype 1a and 1b virus infectivity when compared to the parent series. The details of these findings will be described.

Novel hepatitis C virus entry inhibitors, part 4: The discovery of acyclic acylsulfonamide-bearing triazines as potent HCV entry inhibitors

245th National Meeting (2013)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.