Dominianni S J, Yen T T
Lilly Research Laboratory, Indianapolis, Indiana 46285.
J Med Chem. 1989 Oct;32(10):2301-6. doi: 10.1021/jm00130a013.
Blood glucose levels in viable, yellow, obese, diabetic mice are reduced following oral administration of phenacylimidazolium halides. Compounds 2 and 3 produced reductions of ca. 40% 2 h after doses of 100 mg/kg po. Since these mice do not respond to sulfonylureas, the glucose-lowering activity of phenacylimidazolium salts in this model suggests a mechanism other than that of stimulating insulin secretion. Only phenacylimidazolium halides with electron-donating groups were active; other azolium salts or variations in the phenacyl portion (alterations in the keto function; chain lengthening or extensive branching) produced inactive compounds.
对存活的、黄色的、肥胖的糖尿病小鼠口服卤化苯甲酰咪唑鎓后，其血糖水平会降低。化合物2和3在口服100mg/kg剂量2小时后可使血糖降低约40%。由于这些小鼠对磺酰脲类药物无反应，因此该模型中苯甲酰咪唑鎓盐的降糖活性表明其作用机制并非刺激胰岛素分泌。只有带有供电子基团的卤化苯甲酰咪唑鎓具有活性；其他唑鎓盐或苯甲酰部分的变化（酮功能的改变；链延长或广泛分支）产生的化合物无活性。
