Synthesis and biological evaluation of sulfonylurea and thiourea derivatives substituted with benzenesulfonamide groups as potential hypoglycemic agents
作者:Hui-bin Zhang、Ya-an Zhang、Guan-zhong Wu、Jin-pei Zhou、Wen-long Huang、Xiao-wen Hu
DOI:10.1016/j.bmcl.2009.01.082
日期:2009.3
A novel class of sulfonylurea and thiourea derivatives substituted with benzenesulfonamide groups were designed and synthesized. The target compounds were assayed for the effects on the insulin release of isolated rat pancreatic islets and the glucose transport in adipocytes of rats. Some of them exhibited high potency. Compound 10 also had potent antiplatelet activity and showed an excellent property
设计并合成了一类新型的被苯磺酰胺基取代的磺酰脲和硫脲衍生物。测定目标化合物对离体大鼠胰岛的胰岛素释放和大鼠脂肪细胞中葡萄糖转运的影响。其中一些表现出很高的效力。化合物10还具有强大的抗血小板活性,并且在保护胶原蛋白-肾上腺素诱导的小鼠死亡率以及降低体内血浆葡萄糖活性方面显示出优异的性能。化合物10的初步药理作用表明,它可用于治疗患有心血管和肾病并发症的糖尿病患者。