Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides.
Bioorg Med Chem Lett
; 10(18): 2111-4, 2000 Sep 18.
Article
en En
| MEDLINE
| ID: mdl-10999482
ABSTRACT
Compounds containing a 1,2,3-triazole-substituted benzenesulfonamide were prepared and found to be potent and selective human beta3-adrenergic receptor agonists. The most interesting compound, trifluoromethylbenzyl analogue 12e (beta3 EC50 = 3.1 nM with >1500-fold selectivity over binding to both beta1- and beta2 receptors), stimulates lipolysis in the rhesus monkey (ED50 = 0.36 mg/kg) and is 25% orally bioavailable in the dog.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Agonistas de Receptores Adrenérgicos beta 3
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2000
Tipo del documento:
Article
País de afiliación:
Estados Unidos