Design, synthesis and antidiabetic activity of novel tetrahydrocarboline PPAR regulators / 药学学报
Acta Pharmaceutica Sinica
; (12): 490-496, 2014.
Article
ي Zh
| WPRIM
| ID: wpr-245057
المكتبة المسؤولة:
WPRO
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.
النص الكامل:
1
الفهرس:
WPRIM
الموضوع الرئيسي:
Pharmacology
/
Pyrimidines
/
Structure-Activity Relationship
/
Carbolines
/
Transfection
/
Drug Design
/
Molecular Structure
/
Cells, Cultured
/
Chemistry
/
Thiazolidinediones
المحددات:
Animals
اللغة:
Zh
مجلة:
Acta Pharmaceutica Sinica
السنة:
2014
نوع:
Article