Coumarins hinged directly on benzimidazoles and their ribofuranosides to inhibit hepatitis C virus.
Basic Information
ID: ALA2375297
Journal: Eur J Med Chem
Title: Coumarins hinged directly on benzimidazoles and their ribofuranosides to inhibit hepatitis C virus.
Authors: Tsay SC, Hwu JR, Singha R, Huang WC, Chang YH, Hsu MH, Shieh FK, Lin CC, Hwang KC, Horng JC, De Clercq E, Vliegen I, Neyts J.
Abstract: A new compound library that contained 20 hinged benzimidazole-coumarin hybrids and their β-d-ribofuranosides was established. The anti-hepatitis C virus (HCV) activity of all novel coumarin derivatives, which were obtained by use of organic synthetic methods, was tested. Two of these hybrids exhibited appealing EC50 values of as low as 3.0 and 5.5 μM. The best selectivity index was 14. The incorporation of a d-ribofuranose into the hinged hybrids provided the corresponding nucleosides with the β configuration, one of which inhibited HCV replication with an EC50 value of 20 μM. Additionally, the structure-activity relationship is elucidated on the basis of the functional groups that were attached to the nuclei of benzimidazole, coumarin, and ribofuranose of the hybrids.
CiteXplore: 23501114
DOI: 10.1016/j.ejmech.2013.02.008
Patent ID: ┄