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Bioorg Med Chem Lett. 2009 Feb 1;19(3):627-32. doi: 10.1016/j.bmcl.2008.12.068. Epub 2008 Dec 24.

Tetracyclic indole inhibitors of hepatitis C virus NS5B-polymerase.

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  • 1Department of Medicinal Chemistry, Istituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A., Merck Research Laboratories Rome, 00040 Pomezia, Italy. ian_stansfield@merck.com


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 compounds endowed with good intrinsic enzyme affinity and cell-based potency, as well as superior DMPK profiles to their acyclic counterparts, and ultimately to the identification of a pre-clinical candidate with an excellent predicted human pharmacokinetic profile.

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