Discovery of selective 2, 4-diaminoquinazoline toll-like receptor 7 (TLR 7) agonists
S Pieters, D McGowan, F Herschke, F Pauwels… - Bioorganic & Medicinal …, 2018 - Elsevier
Bioorganic & Medicinal Chemistry Letters, 2018•Elsevier
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.
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.
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.
Elsevier
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