Document Report Card
Basic Information
ID: ALA4428063
Journal: J Med Chem
Title: Novel Pyrimidine Toll-like Receptor 7 and 8 Dual Agonists to Treat Hepatitis B Virus.
Authors: McGowan D, Herschke F, Pauwels F, Stoops B, Last S, Pieters S, Scholliers A, Thoné T, Van Schoubroeck B, De Pooter D, Mostmans W, Khamlichi MD, Embrechts W, Dhuyvetter D, Smyej I, Arnoult E, Demin S, Borghys H, Fanning G, Vlach J, Raboisson P.
Abstract: Toll-like receptor (TLR) 7 and 8 agonists can potentially be used in the treatment of viral infections and are particularly promising for chronic hepatitis B virus (HBV) infection. An internal screening effort identified a pyrimidine Toll-like receptor 7 and 8 dual agonist. This provided a novel alternative over the previously reported adenine and pteridone type of agonists. Structure-activity relationship, lead optimization, in silico docking, pharmacokinetics, and demonstration of ex vivo and in vivo cytokine production of the lead compound are presented.
CiteXplore: 27513093