香豆素-7-磺酰脲类化合物的合成及降血糖活性研究

Synthesis of Coumarin-7-sulfonylurea and Study on its Hypoglycemic Activity

关键词:  香豆素-7-磺酰脲  合成  降血糖活性

Key words:  coumarin-7-sulfonylureas  synthesis  hypoglycemic activity

摘要:

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2 h和4 h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)。

Abstract:

OBJECTIVE To search some new compounds which have hypoglycemic activities. METHODS Novel coumarin-7-sulfonylurea compounds were designed and synthesized by combining the active moieties of hypoglycemic drugs. Their hypoglycemic activities were evaluated in mice. RESULTS These 6 targeted compounds were synthesized and characterized by FT-IR, 1H-NMR and MS spectra. CONCLUSION The preliminary results showed that MSU-3 exhibited evident hypoglycemic effect (P<0.01, CMC-Na as negative control) at the dose of 50 mg·kg^-1, suggesting the promising potential for further investigation.