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Design, synthesis and phenotypic evaluation of N-biaryl amides for IL-17A suppression
A series of N-biaryl amides for Th17 cell phenotypic screening were designed and quickly prepared by microwave-assisted solid-phase organic synthesis. The structure-activity relationship of the three regions of the amides was explored and potent small molecular inhibitors that suppress IL-17A production in mouse Th17 cells were identified. Compound 6h showed excellent suppression of IL-17A with an IC50 of 13 nM, which can be employed as a chemical tool for target identification and Th17 cell-related biological studies.
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Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem