Acute kidney injury (AKI) is associated with a strong inflammatory response, and inhibiting the response effectively prevents or ameliorates AKI. A series of novel arylpropionic esters were designed, synthesized and evaluated their biological activity in LPS-stimulated RAW264.7 cells. Novel arylpropionic esters bearing multi-functional groups showed significant anti-inflammatory activity, in which, compound 13b exhibited the most potent activity through dose-dependent inhibiting the production of nitric oxide (NO, IC₅₀ = 3.52 μM), TNF-α and IL-6 (84.1% and 33.6%, respectively), as well as suppressing the expression of iNOS, COX-2 and TLR4 proteins. In C57BL/6 mice with cisplatin-induced AKI, compound 13b improved kidney function, inhibited inflammatory development, and reduced pathological damage of kidney tissues. In brief, this arylpropionic ester scaffold may be developed as anti-inflammatory agents.

急性肾损伤（AKI）与强烈的炎症反应相关，抑制该反应可有效预防或改善AKI。设计，合成和评估了一系列新颖的芳基丙酸酯在LPS刺激的RAW264.7细胞中的生物学活性。带有多个官能团的新型芳基丙酸酯显示出显着的抗炎活性，其中化合物13b通过剂量依赖性抑制一氧化氮（NO，IC ₅₀  = 3.52μM），TNF-α和IL的产生而表现出最有效的活性。-6（分别为84.1％和33.6％），以及抑制iNOS，COX-2和TLR4蛋白的表达。在具有顺铂诱导的AKI的C57BL / 6小鼠中，化合物13b改善肾脏功能，抑制炎症发展，并减少肾脏组织的病理损伤。简而言之，该芳基丙酸酯支架可以开发为抗炎剂。