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 50 = 268.29 µ m) and glipizide (IC 50 = 300.47 µ m ). The preliminary structure-activity relationships (SARs) of the synthesized compounds were also investigated.

中文翻译：

---

磺酰脲类衍生物的α-葡萄糖苷酶抑制活性的合成与评价

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）。