Synthesis and investigation on antidiabetic activity of 4-(1-aryl-3-oxo-5-phenylpentylamino) benzenesulfonamide / 药学学报
Acta Pharmaceutica Sinica
;
(12): 66-71, 2010.
Article
Dans Chinois
| WPRIM
| ID: wpr-250618
ABSTRACT
Searching for new antidiabetic lead compound, 4-(1-aryl-3-oxo-5-phenylpentylamino) benzenesulfonamides were designed and synthesized directly by three component one-pot condensation of 4-phenyl-2-butanone and sulfanilamide with some aromatic aldehydes at an yield of 23%-97%. The chemical structures of the twelve new Mannich bases were confirmed by 1H NMR, 13C NMR, FTIR, ESI-MS and HR-MS. The screening results of antidiabetic activity indicated that most of these title compounds possess alpha-glucosidase inhibitory activity, among which compound le is the strongest one. And compound 11 possesses good peroxisome proliferator-activated receptor response element (PPRE) agonist activity. The structure-activity relationship of these new beta-amino ketones containing benzenesulfonamide unit was also discussed preliminarily.
Texte intégral:
Disponible
Indice:
WPRIM (Pacifique occidental)
Sujet Principal:
Pharmacologie
/
Relation structure-activité
/
Sulfamides
/
Sulfonamides
/
Conception de médicament
/
Chimie
/
Récepteurs activés par les proliférateurs de peroxysomes
/
Alpha-Glucosidase
/
Inhibiteurs des glycoside hydrolases
/
Hypoglycémiants
langue:
Chinois
Texte intégral:
Acta Pharmaceutica Sinica
Année:
2010
Type:
Article
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