Synthesis and alpha-glucosidase inhibitory activity of N-(1,5-diaryl-3-pentone-1-yl)-4-aminobenzoic acid / 药学学报
Acta Pharmaceutica Sinica
; (12): 48-55, 2009.
Article
in Zh
| WPRIM
| ID: wpr-232599
Responsible library:
WPRO
ABSTRACT
In order to find highly active antidiabetic lead compound, sixteen 4-aminobenzoic acid derivatives were designed and synthesized directly through Mannich reaction in the solution of ethanol at 15-35 degrees C with facile method, mild reaction condition and high yield (45%-90%). Fifteen of them are new compounds. Their structures were confirmed by 1H NMR, 13C NMR, IR, ESI-MS and HR-MS. Alpha-glucosidase inhibitory activity of these compounds indicated that most of these compounds possess the activity with the order: 2c > 2b > 2h > 1a > 1f. The structure-activity relationship of these 4-aminobenzoic acid derivatives was also discussed.
Full text:
1
Database:
WPRIM
Main subject:
Pharmacology
/
Structure-Activity Relationship
/
Drug Design
/
Molecular Structure
/
Chemistry
/
4-Aminobenzoic Acid
/
Alpha-Glucosidases
/
Para-Aminobenzoates
/
Glycoside Hydrolase Inhibitors
/
Hypoglycemic Agents
Language:
Zh
Journal:
Acta Pharmaceutica Sinica
Year:
2009
Document type:
Article