| Literature DB >> 27513093 |
David McGowan1, Florence Herschke1, Frederik Pauwels1, Bart Stoops1, Stefaan Last1, Serge Pieters1, Annick Scholliers1, Tine Thoné1, Bertrand Van Schoubroeck1, Dorien De Pooter1, Wendy Mostmans1, Mourad Daoubi Khamlichi2, Werner Embrechts1, Deborah Dhuyvetter1, Ilham Smyej1, Eric Arnoult1, Samuël Demin1, Herman Borghys1, Gregory Fanning1, Jaromir Vlach1, Pierre Raboisson1.
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.Entities:
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Year: 2016 PMID： 27513093 DOI： 10.1021/acs.jmedchem.6b00747
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446