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Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human beta3 adrenergic receptor agonists
Journal article   Peer reviewed

Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human beta3 adrenergic receptor agonists

E R Parmee, L L Brockunier, J He, S B Singh, M R Candelore, M A Cascieri, L Deng, Y Liu, L Tota, M J Wyvratt, …
Bioorganic & medicinal chemistry letters, Vol.10(20), pp.2283-2286
10/16/2000
PMID: 11055339

Abstract

Recombinant Proteins - antagonists & inhibitors Peptides - chemistry Amides - chemical synthesis Humans Molecular Conformation Adrenergic beta-Agonists - pharmacology Models, Molecular Receptors, Adrenergic, beta-1 - metabolism Structure-Activity Relationship Receptors, Adrenergic, beta-3 - metabolism Receptors, Adrenergic, beta-2 - metabolism Adrenergic beta-Agonists - chemistry Isoquinolines - chemistry Isoquinolines - pharmacology Peptides - chemical synthesis Adrenergic beta-3 Receptor Antagonists Isoquinolines - chemical synthesis Amides - chemistry Adrenergic beta-Agonists - chemical synthesis Drug Design
Tetrahydroisoquinoline derivatives containing a 4-(hexylureido)benzenesulfonamide were examined as human beta3 adrenergic receptor (AR) agonists. Notably, 4,4-biphenyl derivative 9 was a 6 nM full agonist of the beta3 AR. Naphthyloxy compound 18 (beta3 EC50 = 78 nM) did not activate the beta1 and beta2 ARs at 10 microM, and showed >1000-fold selectivity over binding to the beta1 and beta2 ARs.

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