Design, synthesis and anti-inflammatory evaluation of 3-amide benzoic acid derivatives as novel P2Y14 receptor antagonists

European Journal of Medicinal Chemistry
Zhenguo ZhangCheng Jiang

Abstract

The P2Y14 receptor (P2Y14R) plays a key role in the modulation of inflammatory process, but very few classes of antagonists have been reported. A series of 3-amide benzoic acid derivatives were identified as novel and potent P2Y14R antagonists. The most potent antagonist, 16c, showed comparable activity (IC50 = 1.77 nM) to PPTN, the most potent P2Y14R antagonist reported. Compound 16c demonstrated dramatically improved aqueous solubility and excellent metabolic stability in rat and human microsomes. Investigation of the anti-inflammatory effect of 16c was performed in MSU treated THP-1 cells by flow cytometry, Western Blot and immunofluorescence labeling technology, which exhibited that 16c might be a promising candidate for further research.

Citations

Nov 19, 2020·International Journal of Molecular Sciences·Reece Andrew SophocleousRonald Sluyter
Jul 20, 2021·Future Medicinal Chemistry·Yuyang Wang, Yongtao Duan
Jun 20, 2020·ACS Medicinal Chemistry Letters·Fatma MuftiDaniela Salvemini
Oct 12, 2021·Journal of Enzyme Inhibition and Medicinal Chemistry·Ming BianGong Guo-Hua

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