3-溴代香豆素磺酰脲类化合物的合成及其降血糖活性

Synthesis of 3-Bromine-6-sulfonylure a-coumarin and Study on Its Hypoglycemic Activity

目的 :合成新的溴代香豆素磺酰脲类化合物 ,寻找新型降血糖化合物。方法 :运用拼合原理 ,以具有降血糖活性的香豆素为母环 ,在其结构中引入溴和磺酰脲基团并测定目标化合物对小鼠的降血糖活性。结果和结论 :合成了 13个溴代香豆素磺酰脲类化合物 (BSU 1～BSU 13) ,所有目标化合物均未见文献报道 ,其结构经IR、1HNMR和MS鉴定。初步药理实验表明 :化合物BSU 1,BSU 2 ,BSU 3在 2h和 4h对正常小鼠都有明显的降血糖作用 (P <0 . 0 1,与 0 . 5 %CMC Na组比较 )。

AIM:To Synthesize a series compounds of 3-bromine-6-sulfonylurea-coumarin, from which to search for new antidiabetic drugs.METHOD:Bromine and sulfonylurea functional groups were introduced into the structure of coumarin,and the hypoglycemic activity of the target compounds was investigated. RESULT and CONCLUSION:A series of 3-bromine-6-sulfonylurea-coumarin (BSU-1～BSU-13)were firstly synthesized. Their structures were confirmed by IR, 1H NMR and MS. The pharmacological study showed that BSU-1,BSU-2 and BSU-3 exhibited evident hypoglycemic activities (P<0.01,compared with that of 0.5% CMC-Na) at the dose of 50 mg/kg.