Design, synthesis and antidiabetic activity of novel tetrahydrocarboline PPAR regulators / 药学学报
Acta Pharmaceutica Sinica
;
(12): 490-496, 2014.
Article
Dans Chinois
| WPRIM
| ID: wpr-245057
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.
Texte intégral:
Disponible
Indice:
WPRIM (Pacifique occidental)
Sujet Principal:
Pharmacologie
/
Pyrimidines
/
Relation structure-activité
/
Carbolines
/
Transfection
/
Conception de médicament
/
Structure moléculaire
/
Cellules cultivées
/
Chimie
/
Thiazolidinediones
Limites du sujet:
Animaux
langue:
Chinois
Texte intégral:
Acta Pharmaceutica Sinica
Année:
2014
Type:
Article
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