AI Article Synopsis
- A new series of potent quinazoline compounds that activate TLR 7/8 has been discovered and described.
- The research presents the synthesis process and how structural changes can enhance the activity and selectivity for TLR 7.
- Compound 48 was identified as a strong candidate for inducing endogenous interferon (IFN-α) in mice and is effective when taken orally.
Article 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.
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| http://dx.doi.org/10.1016/j.bmcl.2018.01.014 | DOI Listing |
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