多羟基磺胺席夫碱对碳酸酐酶抑制活性的研究

摘要

Sulfanilamide Schiff bases were relatively effective carbonic anhydrase inhibitors （CAIs）, but there are few studies on polyhydroxy sulfanilamide Schiff bases. 18 compounds were designed and syuthesized with microwave-assisted synthesis. Their inhibitory activities were evaluated by determining their IC50 of bCA in order to find out the influence of hydroxyl group to the CAIs activity. The results demonstrated that the control compound （compound 5） had relatively week activity with the ICso 〉20 μmol.L-1, and most of other compounds had IC50 〈5 gmol-L＂t. Especially, Compound 3 was found to be the most effective inhibitor with the IC50 value of 0.86 μmol.L-1. We found that the position and number of hydroxyl group had great influence to the CAIs activity.%磺胺席夫碱是较好的碳酸酐酶抑制剂，然丽对于多羟基磺胺席夫碱的抑制活性研究较少。文章采用微波辅助合成法设计合成了18种多羟基磺胺席夫碱，通过测定该系列化合物对牛碳酸酐酶活性半抑制浓度来评定其抑制活性，探索化合物分子中羟基对碳酸酹酶催化活性的影响。结果表明，对照的4－羟基苯甲醛-4－氨基苯磺酰胺席夫碱（化合物5）对牛红细胞碳酸酐酶的IC50值〉20μmol·L^-1，大部分的席夫碱的IC50值均〈5μmol.L^-1，其中2,4，6-三羟基苯甲醛-4-氨基苯磺酰胺席夫碱（化合物3）的IC59值达到0．86μmol·L^-1，说明磺胺类席夫碱分子结构上羟基的数日和位置对抑制活性有明显的影响。