Design, synthesis, and PPARalpha/gamma agonistic activity of novel tetrahydroisoquinoline derivatives / 药学学报
Acta Pharmaceutica Sinica
;
(12): 311-316, 2011.
Article
in Chinese
| WPRIM
| ID: wpr-348959
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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Structure-Activity Relationship
/
Transfection
/
Drug Design
/
Chemistry
/
Tetrahydroisoquinolines
/
PPAR alpha
/
PPAR gamma
/
HEK293 Cells
/
Hypoglycemic Agents
Limits:
Humans
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2011
Type:
Article
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