建立了毛细管区带电泳技术快速测定D1蛋白酶活性及其抑制剂先导化合物的筛选方法。实验选用未涂层熔融石英毛细管(43 cm 5mm)和磷酸盐缓冲溶液(50 mmol/L, pH 3.0)作为分离介质,运行电压18 kV,测定了D1蛋白酶的活性并对部分抑制剂先导化合物进行了筛选。结果表明, ITP26和ITP21两种异噁唑噻唑哌啶类先导化合物对蛋白酶活性具有抑制作用,抑制率分别为26%和13%。 A capillary zone electrophoresis technique was developed to rapidly determine the activity of D1 protease and its screening method for the lead compounds as inhibitors. In the experiment, uncoated fused silica capillary (43 cm 5 mm) and phosphate buffer solution (50 mmol / L, pH 3.0) were used as the separation media. The voltage was 18 kV. The activity of D1 protease was measured and some inhibitor precursor compounds The screening. The results showed that the two isoxazole thiazolyl piperidine precursors of ITP26 and ITP21 had an inhibitory effect on the protease activity with the inhibition rates of 26% and 13%, respectively.