Related Experiment Video
Updated: Jun 26, 2026

A Competent Hepatocyte Model Examining Hepatitis B Virus Entry through Sodium Taurocholate Cotransporting Polypeptide as a Therapeutic Target
Published on: May 10, 2022
Tetracyclic indole inhibitors of hepatitis C virus NS5B-polymerase
Ian Stansfield1, Caterina Ercolani, Angela Mackay
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
Abstract:
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.
Related Concept Videos
Antiviral Nucleoside Inhibitors
Inhibitors of Viral Protein Synthesis
Inhibitors Of Virion Release
Inhibitors of Virion Maturation and Assembly
Hepatitis
Inhibitors of Bacterial DNA Synthesis

