Design and synthesis of tetrahydropyridopyrimidine based Toll-Like Receptor (TLR) 7/8 dual agonists

Bioorganic & Medicinal Chemistry Letters
David McGowanPierre Raboisson

Abstract

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.

Citations

Jan 11, 2020·Frontiers in Immunology·Monica C GestalEric T Harvill
Nov 27, 2019·Current Topics in Medicinal Chemistry·David C McGowan
Mar 24, 2020·European Journal of Medicinal Chemistry·Cindy PatinoteCarine Deleuze-Masquéfa
Mar 28, 2021·European Journal of Medicinal Chemistry·Jingyu ZhangXiaowu Dong
Aug 7, 2021·RSC Medicinal Chemistry·Deepender KaushikDeepak B Salunke
Sep 12, 2020·Chemical Reviews·Wen-Hao Li, Yan-Mei Li

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