Design, synthesis, and PPARalpha/gamma agonistic activity of novel tetrahydroisoquinoline derivatives.
- Author:
Ran YU
;
Yanli ZHOU
;
Yi HUAN
;
Quan LIU
;
Zhufang SHEN
;
Zhanzhu LIU
- Publication Type:Journal Article
- From:
Acta Pharmaceutica Sinica
2011;46(3):311-6
- CountryChina
- Language:Chinese
-
Abstract:
A series of tetrahydroisoquinoline derivatives were prepared and their peroxisome proliferator-activated receptor (PPAR) alpha/gamma 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 PPARgamma than that of the comparison, six compounds exhibited higher agonistic activities of PPARalpha than that of the comparison, and compound 8a was discovered as a highly potent PPARalpha/gamma 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.
