CARBOXYL-PROMOTED ENHANCEMENT OF SELECTIVITY FOR THE BETA(3) ADRENERGIC-RECEPTOR - NEGATIVE CHARGE OF THE SULFONIC-ACID BMS-187413 INTRODUCES BETA(3) BINDING SELECTIVITY

Authors
SHER PM MATHUR A FISHER LG WU G SKWISH S MICHEL IM SEILER SM DICKINSON KEJ
Citation
Pm. Sher et al., CARBOXYL-PROMOTED ENHANCEMENT OF SELECTIVITY FOR THE BETA(3) ADRENERGIC-RECEPTOR - NEGATIVE CHARGE OF THE SULFONIC-ACID BMS-187413 INTRODUCES BETA(3) BINDING SELECTIVITY, Bioorganic & medicinal chemistry letters, 7(12), 1997, pp. 1583-1588
Citations number
31
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
12
Year of publication
1997
Pages
1583 - 1588
Database
ISI
SICI code
0960-894X(1997)7:12<1583:CEOSFT>2.0.ZU;2-M
Abstract
Carboxyl and other negatively charged groups were found to be most eff ective at producing human beta(3) adrenergic receptor binding selectiv ity in 1 (BRL 37344) and related compounds. The sulfonic acid analog 7 (BMS-187413) is a novel and potent beta(3) adrenergic agonist that bi nds selectively, and thus has an in vitro profile that compares favora bly with that of BRL 37344. (C) 1997 Elsevier Science Ltd.