Synthesis and evaluation of <i>α</i>-glucosidase inhibitory activity of sulfonylurea derivatives
作者:Thi Thoi Bui、Van Loc Tran、Dai Quang Ngo、Van Chien Tran、Van Sung Tran、Thi Phuong Thao Tran
DOI:10.1515/znb-2020-0134
日期:2021.4.27
Two series of sulfonylureas derivatives including 24 compounds ( 4 , 7 , 5a – 5o , 8a – 8h ), among them 17 new derivatives, have been synthesized and evaluated for their α -glucosidase inhibitory activity. Compounds 5c , 5h and 8e showed significant in vitro α -glucosidase inhibition with IC 50 values of 5.58, 79.85 and 213.36 µ m , respectively, comparing with the standard compounds acarbose (IC
合成了两个系列的磺酰脲类衍生物,包括24种化合物(4、7、5a-5o,8a-8h),其中包括17种新衍生物,并评估了它们对α-葡萄糖苷酶的抑制活性。与标准化合物阿卡波糖(IC 50 = 268.29 µm)和格列吡嗪(IC 50 = 300.47)相比,化合物5c,5h和8e在体外具有明显的α-葡萄糖苷酶抑制作用,IC 50值分别为5.58、79.85和213.36 µm。 )。还研究了合成化合物的初步结构-活性关系(SAR)。