文档介绍：萘啶衍生物的合成及其醛糖还原酶抑制活性研究
杜蕊,朱长进收稿日期:2008 - 9 -
作者简介:杜蕊(1983—),女,博士研究生
*通讯作者:朱长进(1958—),男,教授,E-mail: ******@bit.
(北京理工大学化工与环境学院,北京,100081)
摘要:目的开发一系列带有新型结构的醛糖还原酶抑制剂。方法基于几种已存在的醛糖还原酶抑制剂的结构,经过4步反应,合成了三种萘啶衍生物,并对其进行体外ALR2活性测试。结果三种化合物表现出了一定的酶抑制活性,并且三者活性值相近。结论萘啶化合物的结构骨架合理,经过改进或修饰可能会提高活性。
关键词:醛糖还原酶抑制剂;萘啶;抑制活性
Synthesis of Naphthyridine Derivatives and Research of their Aldose Reductase Inhibitory Activity
DU Rui, ZHU Chang-jin
(School of Chemical Engineering and Environment , Beijing Institute of Technology , Beijing 100081 , China)
Abstract: Objective A series of aldose reductase inhibitors (ARIs) with new structures have been developed. Methods Based on several ARIs existed, three naphthyridine derivatives have been designed and synthesized via four steps of reaction, and the ALR2 activity of them three were tested. Results The pounds showed a certain inhibitory activity, and the data of their activity were similar. Conclusion The bone structure of pound was reasonable, the activity might be better if the structure of pound was improved or modified.
Key words: aldose reductase inhibitors; naphthyridine; inhibitory activity
糖尿病(diabetes mellitus,DM)是一组以持续高血糖为主要特征的代谢综合征。随着人民生活水平的日益提高, 糖尿病患病率有急剧增加的趋势,已成为影响人类身体健康的常见疾病之一。大量研究证实, 糖尿病并发症是由于糖尿病患者体内多元醇代谢通路异常致使体内山梨醇蓄积造成。大量动物实验和临床研究表明醛糖还原酶抑制剂(aldose reductase inhibitors, ARIs) 可有效改善糖尿病患者多元醇代谢通路异常, 从而达到预防和延缓糖尿病并发症的产生[1]。因此,寻找高效低毒的治疗糖尿病并发症药