951174-17-7Relevant articles and documents
Novel Pyrimidine Toll-like Receptor 7 and 8 Dual Agonists to Treat Hepatitis B Virus
McGowan, David,Herschke, Florence,Pauwels, Frederik,Stoops, Bart,Last, Stefaan,Pieters, Serge,Scholliers, Annick,Thoné, Tine,Van Schoubroeck, Bertrand,De Pooter, Dorien,Mostmans, Wendy,Khamlichi, Mourad Daoubi,Embrechts, Werner,Dhuyvetter, Deborah,Smyej, Ilham,Arnoult, Eric,Demin, Samu?l,Borghys, Herman,Fanning, Gregory,Vlach, Jaromir,Raboisson, Pierre
supporting information, p. 7936 - 7949 (2016/11/07)
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.