Discovery of conformationally constrained tetracyclic compounds as potent hepatitis C virus NS5B RNA polymerase inhibitors.
Basic Information
ID: ALA1137351
Journal: J Med Chem
Title: Discovery of conformationally constrained tetracyclic compounds as potent hepatitis C virus NS5B RNA polymerase inhibitors.
Authors: Ikegashira K, Oka T, Hirashima S, Noji S, Yamanaka H, Hara Y, Adachi T, Tsuruha J, Doi S, Hase Y, Noguchi T, Ando I, Ogura N, Ikeda S, Hashimoto H.
Abstract: We report a new series of hepatitis C virus NS5B RNA polymerase inhibitors containing a conformationally constrained tetracyclic scaffold. SAR studies led to the identification of 6,7-dihydro-5H-benzo[5,6][1,4]diazepino[7,1-a]indoles (19 and 20) bearing a basic pendent group with high biochemical and cellular potencies. These compounds displayed a very small shift in cellular potency when the replicon assay was performed in the presence of human serum albumin.
CiteXplore: 17125247
DOI: 10.1021/jm0610245
Patent ID: ┄