当前位置: X-MOL 学术Bioorg. Med. Chem. Lett. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Discovery of selective 2,4-diaminoquinazoline toll-like receptor 7 (TLR 7) agonists
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2018-01-16 , DOI: 10.1016/j.bmcl.2018.01.014
Serge Pieters , David McGowan , Florence Herschke , Frederik Pauwels , Bart Stoops , Stefaan Last , Werner Embrechts , Annick Scholliers , Wendy Mostmans , Kris Van Dijck , Bertrand Van Schoubroeck , Tine Thoné , Dorien De Pooter , Gregory Fanning , Mari Luz Rosauro , Mourad Daoubi Khamlichi , Ioannis Houpis , Eric Arnoult , Tim H.M. Jonckers , Pierre Raboisson

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.



中文翻译:

发现选择性的2,4-二氨基喹唑啉Toll样受体7(TLR 7)激动剂

描述了发现一系列新型的高效喹唑啉TLR 7/8激动剂。提出了合成和结构-活性关系。对TLR 7选择性的结构要求和该系列的优化提供了有效的激动剂48。药代动力学和药效学研究突出了48种小鼠中可口服的内源性干扰素(IFN-α)诱导剂。

更新日期:2018-01-16
down
wechat
bug