化学
兴奋剂
佐剂
疫苗佐剂
Toll样受体
受体
体内
药理学
先天免疫系统
免疫学
生物化学
医学
生物
生物技术
作者
David McGowan,Florence Herschke,Mourad Daoubi Khamlichi,Mari Luz Rosauro,Sara M. Pérez Benedicto,Frederik Pauwels,Bart Stoops,Vineet Pande,Annick Scholliers,Bertrand Van Schoubroeck,Wendy Mostmans,Kris Van Dijck,Tine Thoné,Helen Horton,Gregory Fanning,Tim H. M. Jonckers,Pierre Raboisson
标识
DOI:10.1016/j.bmcl.2018.08.015
摘要
In a continuing effort to discover novel TLR agonists, herein we report on the discovery and structure-activity relationship of novel tetrahydropyridopyrimidine TLR 7/8 agonists. Optimization of this series towards dual agonist activity and a high clearance profile resulted in the identification of compound 52a1. Evaluation in vivo revealed an interferon stimulated response (ISG) in mice with limited systemic exposure and demonstrated the potential in antiviral treatment or as a vaccine adjuvant.
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