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Identification of Human Toll-like Receptor 2-Agonistic Activity in Dihydropyridine-Quinolone Carboxamides.

ABSTRACT: 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.

SUBMITTER: Hu Z 

PROVIDER: S-EPMC6331173 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature

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Identification of Human Toll-like Receptor 2-Agonistic Activity in Dihydropyridine-Quinolone Carboxamides.

Hu Ziwei Z   Banothu Janardhan J   Beesu Mallesh M   Gustafson Collin J CJ   Brush Michael J H MJH   Trautman Kathryn L KL   Salyer Alex C D ACD   Pathakumari Balaji B   David Sunil A SA  

ACS medicinal chemistry letters 20181220 1

Using a multiplexed, reporter gene-based, high-throughput screen, we identified 9-fluoro-7-hydroxy-3-methyl-5-oxo-<i>N</i>-(pyridin-3-ylmethyl)-2,3-dihydro-1<i>H</i>,5<i>H</i>-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. ...[more]

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