| Literature DB >> 29366653 |
Serge Pieters1, David McGowan2, Florence Herschke2, Frederik Pauwels2, Bart Stoops2, Stefaan Last2, Werner Embrechts2, Annick Scholliers2, Wendy Mostmans2, Kris Van Dijck2, Bertrand Van Schoubroeck2, Tine Thoné2, Dorien De Pooter2, Gregory Fanning2, Mari Luz Rosauro3, Mourad Daoubi Khamlichi3, Ioannis Houpis2, Eric Arnoult4, Tim H M Jonckers2, Pierre Raboisson2.
Abstract
The discovery of a novel series of highly potent quinazoline TLR 7/8 agonists is described. The synthesis and structure-activity relationship is presented. Structural requirements and optimization of this series toward TLR 7 selectivity afforded the potent agonist 48. Pharmacokinetic and pharmacodynamic studies highlighted 48 as an orally available endogenous interferon (IFN-α) inducer in mice.Entities:
Keywords: HBV; Quinazoline; TLR7
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Year: 2018 PMID： 29366653 DOI： 10.1016/j.bmcl.2018.01.014
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823