Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides.
Bioorg Med Chem Lett
; 10(18): 2111-4, 2000 Sep 18.
Article
in 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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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Adrenergic beta-3 Receptor Agonists
Limits:
Animals
/
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2000
Document type:
Article
Affiliation country:
United States