Design, synthesis and antidiabetic activity of novel tetrahydrocarboline PPAR regulators.
- Author:
Kun PENG
;
Yi HUAN
;
Quan LIU
;
Zhu-Fang SHEN
;
Zhan-Zhu LIU
- Publication Type:Journal Article
- MeSH:
Animals;
Carbolines;
chemical synthesis;
chemistry;
pharmacology;
Cells, Cultured;
Drug Design;
Hypoglycemic Agents;
chemical synthesis;
chemistry;
pharmacology;
Molecular Structure;
PPAR alpha;
agonists;
PPAR gamma;
agonists;
Peroxisome Proliferator-Activated Receptors;
agonists;
Pyrimidines;
metabolism;
Structure-Activity Relationship;
Thiazolidinediones;
metabolism;
Transfection
- From:
Acta Pharmaceutica Sinica
2014;49(4):490-496
- CountryChina
- Language:Chinese
-
Abstract:
A series of novel tetrahydrocarboline derivatives was designed and synthesized in order to discover more potent peroxisome proliferator-activated receptor (PPAR) alpha/gamma dual regulators. The structures of these compounds were confirmed by 1H NMR and HR-MS; their PPAR-regulating activities were evaluated in vitro. Compounds 6h, 6n, 6p and 6q exhibited more potent PPARalpha agonistic activities than the control drug WY14643, while compounds 60, 6g, 6i and 6q exhibited more potent PPARgamma agonistic activities than the control drug rosiglitazone. Compound 6q was discovered as a potent PPARalpha/gamma dual agonist and deserves further investigation.
