Discovery of Conformationally Constrained Tetracyclic Compounds as Potent Hepatitis C Virus NS5B RNA Polymerase Inhibitors
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- 作者：Kazutaka Ikegashira ; Takahiro Oka ; Shintaro Hirashima ; Satoru Noji ; Hiroshi Yamanaka ; Yoshinori Hara ; Tsuyoshi Adachi ; Jun-Ichiro Tsuruha ; Satoki Doi ; Yasunori Hase ; Toru Noguchi ; Izuru Ando ; Naoki Og
- 刊名：Journal of Medicinal Chemistry
- 出版年：2006
- 出版时间：November 30, 2006
- 年：2006
- 卷：49
- 期：24
- 页码：6950 - 6953
- 全文大小：167K
- 年卷期：v.49,no.24(November 30, 2006)
- ISSN：1520-4804
文摘
We report a new series of hepatitis C virus NS5B RNApolymerase inhibitors containing a conformationally constrainedtetracyclic 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 basicpendent group with high biochemical and cellular potencies. Thesecompounds displayed a very small shift in cellular potency when thereplicon assay was performed in the presence of human serum albumin.