摘要
目的合成新的多取代香豆素磺酰脲类化合物。方法运用骈合原理 ,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效果。结果与结论合成了 13个多取代香豆素磺酰脲类化合物 (BMSU 1～BMSU 13) ,所有目标化合物均未见文献报道 ,其结构经红外光谱、核磁共振氢谱和质谱确证。初步药理实验表明 :目标化合物BMSU 3、BMSU 4、BMSU 5、BMSU 9、BMSU 10对正常小鼠都有明显的降血糖作用 (P <0 0 1)。
Aim To search for new antidiabetic drugs.Methods Bromine and sulfonylurea functional groups were introduced into the structure of coumarin,and the hypoglycemic activity of the target compounds was measured.Results and conclusion A series of coumarin 6 sulfonylureas(BMSU 1～BMSU 13)were synthesized and their structures were identified by IR, 1H NMR and MS spectra never reported.The pharmacological study showed that BMSU 3,BMSU 4,BMSU 5,BMSU 9,BMSU 10 exhibited evident hypoglycemic activity( P <0.01)at the dose of 50 mg/kg.
出处
《中国药物化学杂志》
CAS
CSCD
2004年第6期331-334,共4页
Chinese Journal of Medicinal Chemistry
关键词
药物化学
制备
化学合成
香豆素磺酰脲
降血糖
medicinal chemistry
preparation
chemical synthesis
coumarins-6-sulfonylureas
hypoglycemic
