药学学报, 2011, 46(3): 311-316
引用本文:
于 然 周艳丽 环 奕 刘 泉 申竹芳 刘站柱. 一类新型的四氢异喹啉类PPARα/γ受体激动剂的设计、合成与活性研究[J]. 药学学报, 2011, 46(3): 311-316.
XU Ran, Zhou-Yan-Li, Huan- Yi, Liu- Quan, Shen-Zhu-Fang, Liu-Zhan-Zhu. Design, synthesis, and PPARα/γ agonistic activity of novel tetrahydroisoquinoline derivatives[J]. Acta Pharmaceutica Sinica, 2011, 46(3): 311-316.

一类新型的四氢异喹啉类PPARα/γ受体激动剂的设计、合成与活性研究
于 然, 周艳丽, 环 奕, 刘 泉, 申竹芳, 刘站柱*
(中国医学科学院、北京协和医学院药物研究所, 北京 100050)
摘要:

为得到更高效的PPAR (过氧化物酶体增殖激活受体) α/γ受体激动剂, 设计合成了新型的四氢异喹啉类化合物, 通过1H NMRHR-MS对化合物结构进行了确证, 并测定了化合物的体外PPARα/γ受体激动活性。其中化合物8a具有PPARα/γ双受体激动活性, PPARα/γ受体激动活性与阳性对照品WY14643、罗格列酮相比活性更强。

关键词:   
Design, synthesis, and PPARα/γ agonistic activity of novel tetrahydroisoquinoline derivatives
Abstract:

A series of tetrahydroisoquinoline derivatives were prepared and their peroxisome proliferator- activated receptor (PPAR) α/γ agonistic activities were evaluated to obtain more potent PPAR agonist.  All of them were new compounds, and their structures were confirmed by 1H NMR and HR-MS.  Three compounds exhibited higher agonistic activities of PPARγ than that of the comparison, six compounds exhibited higher agonistic activities of PPARα than that of the comparison, and compound 8a was discovered as a highly potent PPARα/γ agonist that is much more active than that of WY14643 and rosiglitazone.  The development of potent PPAR agonists may offer a new choice for the treatment of diabetes.

Key words:   
收稿日期:
相关功能
PDF(236KB) Free
打印本文
0
作者相关文章