香豆素-7-磺酰脲类化合物的合成及降血糖活性研究

• 作 者: 祁刚 屠树滋
• 机 构: 盐城工学院化生学院,中国药科大学药物化学教研室,
• 出 处: 中国现代应用药学
• 发表日期: 2010年03期
• 关键词: coumarin-7-sulfonylureas synthesis hypoglycemic activity

目的寻找新型降糖活性的化合物。方法运用拼合原理将磺酰脲类降糖活性化合物的药效团磺酰脲基与有降糖活性的香豆素拼合,设计合成了香豆素磺酰脲类化合物。结果设计并合成了6个新的化合物,该类化合物未见文献报道,结构均经IR、1H-NMR、MS鉴定。结论初步药理实验表明MSU-3在2h和4h对正常小鼠都有明显的降血糖作用(P<0.01,与0.5%CMC-Na组比较)。

Aim To find new hypoglycemic compounds. Methods Combining the pharmacodynamics sulfonylurea of ​​sulfonylurea hypoglycemic compounds with coumarin with hypoglycemic activity, the coumarin sulfonylureas were designed and synthesized. Results Six new compounds were designed and synthesized. These compounds have not been reported in the literature. Their structures were identified by IR, 1H-NMR and MS. Conclusion Preliminary pharmacological experiments show that MSU-3 has obvious hypoglycemic effect on normal mice at 2h and 4h (P <0.01, compared with 0.5% CMC-Na group).