Design, synthesis, and PPARalpha/gamma agonistic activity of novel tetrahydroisoquinoline derivatives.
- Author:
Ran YU
1
;
Yan-Li ZHOU
;
Yi HUAN
;
Quan LIU
;
Zhu-Fang SHEN
;
Zhan-Zhu LIU
Author Information
1. Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
- Publication Type:Journal Article
- MeSH:
Drug Design;
HEK293 Cells;
Humans;
Hypoglycemic Agents;
chemical synthesis;
chemistry;
pharmacology;
PPAR alpha;
agonists;
metabolism;
PPAR gamma;
agonists;
metabolism;
Structure-Activity Relationship;
Tetrahydroisoquinolines;
chemical synthesis;
chemistry;
pharmacology;
Transfection
- From:
Acta Pharmaceutica Sinica
2011;46(3):311-316
- 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.
