N-(1，5-二芳基-3-戊酮-1-基)-4-氨基苯甲酸的合成与α-葡糖苷酶抑制活性初步研究

Synthesis and α-glucosidase inhibitory activity of N-(1,5-diaryl-3-pentone-1-yl)-4-aminobenzoic acid

由Mannich反应直接合成了16个β-氨基酮化合物,制备方法简单、反应条件温和、产品易纯化,收率达到45%～90%。所制备的化合物通过IR、ESI-MS、1H NMR、13C NMR和HR-MS等方法进行了结构表征。α-葡糖苷酶抑制活性检测表明,所合成的化合物对该酶的抑制活性顺序为:2c最强,2b、2h、1a、1f有一定的抑制活性。在此基础上,对合成化合物的构-效关系进行了讨论。

In order to find highly active antidiabetic lead compound, sixteen 4-aminobenzoic acid derivatives were designed and synthesized directly through Mannich reaction in the solution of ethanol at 15-35 ℃ with facile method, mild reaction condition and high yield （45%-90%）. Fifteen of them are new compounds. Their structures were confirmed by ^1H NMR, ^13C NMR, IR, ESI-MS and HR-MS. α-Glucosidase inhibitory activity of these compounds indicated that most of these compounds possess the activity with the order： 2c 〉 2b 〉 2h 〉 1a 〉 If The structure-activity relationship of these 4-aminobenzoic acid derivatives was also discussed.