论文部分内容阅读
基于本实验室前期发现的高活性分子的结构特征,作者设计了含有对氨基苯甲酸和苯磺酰胺结构单元的新型分子.通过4条合成路线的探索,发现了中间体IM1～IM3及目标分子TM1和TM2的简捷合成路线和实用合成方法;采用本实验室前期建立的合成方法,顺利得到设计的26个化合物,合成方法简便,反应条件温和,收率为64%～95%.21个新化合物通过1H NMR,13C NMR和HRMS进行结构表征.目前的体外抗糖尿病活性结果显示,所得26个分子的过氧化物酶体增殖物激活受体(PPAR)的激动活性较弱.本研究进一步证实了醇/二氯亚砜体系脱除脂肪酰芳胺酰基的能力,有助于含有对氨基苯甲酸和苯磺酰胺结构单元分子的进一步结构优化.
Based on the structural features of highly active molecules found in our laboratory, the authors designed novel molecules containing p-aminobenzoic acid and benzenesulfonamide structural units.Through the exploration of four synthetic routes, we found that the intermediates IM1 ~ IM3 and target molecules TM1 and TM2, a simple synthesis route and practical synthesis method; 26 compounds were successfully designed by using the synthesis method preliminarily established in our laboratory, the synthesis method is simple and the reaction conditions are mild with the yield of 64% -95% .21 new The compounds were characterized by 1H NMR, 13C NMR and HRMS.The present in vitro antidiabetic activity results show that the resulting 26 molecules have weaker activation activity of peroxisome proliferator-activated receptor (PPAR) .The study further confirmed The ability of the alcohol / thionyl chloride system to remove fatty acyl-arylaminoacids contributes to the further structural optimization of the molecules containing p-aminobenzoic acid and benzenesulfonamide structural units.