4-[3-(4-溴苯基)-3-氧代-1-芳基丙氨基]-N-(嘧啶-2-基)苯磺酰胺的合成及其α-葡萄糖苷酶抑制活性初步研究

Synthesis and Preliminary Study on α-Glucosidase Inhibitory Activity of 4-[3-(4-Bromophenyl)-3-oxo-1-arylpropylamino]-N-(pyrimidin-2-yl)benzenesulfonamide

为了寻求新颖的抗糖尿病药物,我们将芳香醛、对溴苯乙酮和磺胺嘧啶通过一步反应直接合成了16个未见报道的含有磺胺嘧啶结构的β-氨基酮化合物,制备方法简便、反应条件温和,收率为10.0%～80.1%.所制备的化合物通过1HNMR,13CNMR,MS和HRMS进行结构表征与确证.对这些化合物进行α-葡萄糖苷酶抑制活性初步检测,结果表明部分化合物在低浓度范围(8.1～9.3nmol·mL-1)具有一定的α-葡萄糖苷酶抑制活性.

To explore novel antidiabetic drugs with high efficacy and low toxicity, sixteen new β-amino ketones containing a sulfadiazine moiety have been synthesized through Marmich reaction of sulfadiazine with p-bromoacetophenone and some aromatic aldehydes in the yields of 10.0%-80.1%. Their chemical structures have been confirmed by IR, ^1H NMR,^13C NMR, ESI-MS and HRMS techniques. The preliminary α-glucosidase inhibitory activity bioassay of these compounds indicated that some compounds displayed α-glucosidase inhibitory activity in the low concentration range of 8.1 -9.3 nmol·mL^-1.