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
en Zh
| WPRIM
| ID: wpr-250618
Biblioteca responsable:
WPRO
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.
Texto completo:
1
Índice:
WPRIM
Asunto principal:
Farmacología
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Relación Estructura-Actividad
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Sulfanilamidas
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Sulfonamidas
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Diseño de Fármacos
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Química
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Receptores Activados del Proliferador del Peroxisoma
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Alfa-Glucosidasas
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Inhibidores de Glicósido Hidrolasas
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Hipoglucemiantes
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Año:
2010
Tipo del documento:
Article