目的 設(shè)計合成一類含萘甲基三唑結(jié)構(gòu)的羧酸類化合物，并對其抑制尿酸轉(zhuǎn)運體1（URAT1）的活性進行研究。方法 以4-溴甲基萘、1H-1，2，4-三氮唑-3-硫醇和溴乙酸甲酯為起始原料，通過取代、水解等反應(yīng)合成目標(biāo)化合物，并對其抑制URAT1的活性進行研究。結(jié)果 設(shè)計并合成了3個目標(biāo)化合物，結(jié)構(gòu)經(jīng)¹H-NMR和MS確證?；钚詼y試結(jié)果顯示化合物F-2和G-2具有比陽性對照藥lesinurad還要強的URAT1抑制活性。結(jié)論 設(shè)計了一條合成目標(biāo)化合物的簡易路線，該路線操作簡便、路線短、收率高。目標(biāo)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.

天津市科技支撐計劃重點項目（16YFZCSY00910）