Using a multiplexed, reporter gene-based, high-throughput screen, we identified 9-fluoro-7-hydroxy-3-methyl-5-oxo-N-(pyridin-3-ylmethyl)-2,3-dihydro-1H,5H-pyrido[3,2,1-ij]quinoline-6-carboxamide as a TLR2 agonist. Preliminary structure-activity relationship studies on the carboxamide moiety led to the identification of analogues that induce chemokines and cytokines in a TLR2-dependent manner. These results represent new leads for the development of vaccine adjuvants.
Bibliographical noteFunding Information:
*Phone: (612) 625-3848. E-mail: email@example.com. ORCID Sunil A. David: 0000-0003-1655-4641 Author Contributions ‡These authors contributed equally. Funding This work was supported by NIH/NIAID contract HHSN272201400056C. Notes The authors declare no competing financial interest.
© 2018 American Chemical Society.
- Toll-like receptor 2
- Vaccine adjuvants