目的 设计合成一类含萘甲基三唑结构的羧酸类化合物，并对其抑制尿酸转运体1（URAT1）的活性进行研究。方法 以4-溴甲基萘、1H-1，2，4-三氮唑-3-硫醇和溴乙酸甲酯为起始原料，通过取代、水解等反应合成目标化合物，并对其抑制URAT1的活性进行研究。结果 设计并合成了3个目标化合物，结构经¹H-NMR和MS确证。活性测试结果显示化合物F-2和G-2具有比阳性对照药lesinurad还要强的URAT1抑制活性。结论 设计了一条合成目标化合物的简易路线，该路线操作简便、路线短、收率高。目标化合物也具有一定的生物活性。

Objective To design and synthesize naphthyl triazole carboxylic acid compounds and study their inhibitory activities against URAT1. Methods 4-Bromomethyl-naphthalene, [1,2,4]triazole-3-thiol, and methyl bromoacetate were used as a starting material to synthesize the target compounds by substitution and hydrolysis reaction. And their URAT1 inhibitory activities were tested. Results Three target compounds were designed and synthesized, and their chemical structures were confirmed by ¹H-NMR and MS. Activities test showed that compounds F-2 and G-2 had stronger URAT1 inhibitory activities than positive control drug lesinurad. Conclusion A facile route for synthesis of target compound is developed, which has the advantages of simple operating procedure, easy post-processing, and high-yield. And target compounds have a certain biological activities.

天津市科技支撑计划重点项目（16YFZCSY00910）