917364-95-5Relevant academic research and scientific papers
Tetracyclic indole inhibitors of hepatitis C virus NS5B-polymerase
Stansfield, Ian,Ercolani, Caterina,Mackay, Angela,Conte, Immacolata,Pompei, Marco,Koch, Uwe,Gennari, Nadia,Giuliano, Claudio,Rowley, Michael,Narjes, Frank
scheme or table, p. 627 - 632 (2009/09/06)
We report the evolutionary path from an open-chain series to conformationally constrained tetracyclic indole inhibitors of HCV NS5B-polymerase, where the C2 aromatic is tethered to the indole nitrogen. SAR studies led to the discovery of zwitterionic comp
Discovery of conformationally constrained tetracyclic compounds as potent hepatitis C virus NS5B RNA polymerase inhibitors
Ikegashira, Kazutaka,Oka, Takahiro,Hirashima, Shintaro,Noji, Satoru,Yamanaka, Hiroshi,Hara, Yoshinori,Adachi, Tsuyoshi,Tsuruha, Jun-Ichiro,Doi, Satoki,Hase, Yasunori,Noguchi, Toru,Ando, Izuru,Ogura, Naoki,Ikeda, Satoru,Hashimoto, Hiromasa
, p. 6950 - 6953 (2007/10/03)
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.
