目的设计合成苯并间二氧杂环戊烯-2,2-二羧酸衍生物,并研究其PPARδ激动作用,以期发现新颖的PPARδ激动剂。方法以芳香甲酰胺和邻苯二酚为起始原料,经十余步反应制得目标化合物;并用细胞水平的转染激动实验评价目标化合物的PPARδ激动活性。结果与结论合成目标化合物15个,其结构经核磁和质谱确证。初步生物活性评价结果显示,此类化合物对PPARδ具有一定的激动作用,其中XI-c1的最大激动作用达到阳性对照药GW501516的90%。 OBJECTIVE To design and synthesize benzodioxole-2,2-dicarboxylic acid derivatives and study their PPARδ agonism in order to find new PPARδ agonists. Methods Starting from aromatic formamide and catechol, the target compounds were prepared by more than ten steps reactions. The PPARδ agonistic activity of target compounds was evaluated by cell-level transfection and activation assays. Results and Conclusion Fifteen target compounds were synthesized and their structures were confirmed by NMR and MS. The results of preliminary bioassay showed that these compounds have certain agonism on PPARδ, and the maximal agonism of XI-c1 reached 90% of the positive control GW501516.