Schweizer E H, Märki F, Rihs G
J Med Chem. 1983 Jul;26(7):970-3. doi: 10.1021/jm00361a007.
Hypoglycemic sulfonyliminoimidazolidines were shown to stimulate insulin release in vitro (rabbit pancreas) and in vivo (normal rats) comparable to tolbutamide and to inhibit glucose oxidation in isolated rat fat cells in vitro similar to phenformin. These results support the hypothesis that the hypoglycemic effect of the compounds in normal and in diabetic animals may be due to a combination of mechanisms operative in sulfonylureas and biguanides. Determination of the three-dimensional structure of the potent analogue 1 by X-ray crystallography enabled us to identify specific regions of the molecule presumed to be involved in the molecular mode of action of sulfonyl-iminoimidazolidines.
降糖磺酰亚氨基咪唑烷类化合物在体外（兔胰腺）和体内（正常大鼠）均显示出能刺激胰岛素释放，其效果与甲苯磺丁脲相当；在体外能抑制分离的大鼠脂肪细胞中的葡萄糖氧化，效果与苯乙双胍相似。这些结果支持了这样一种假说，即这些化合物在正常动物和糖尿病动物中的降糖作用可能是由于磺脲类和双胍类药物中起作用的多种机制共同作用的结果。通过X射线晶体学确定强效类似物1的三维结构，使我们能够识别分子中假定参与磺酰亚氨基咪唑烷类分子作用模式的特定区域。
