Design, synthesis and phenotypic evaluation of N-biaryl amides for IL-17A suppression

Abstract

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.