Carboxyl-promoted enhancement of selectivity for the β3 adrenergic receptor. Negative charge of the sulfonic acid BMS-187413 introduces-β3 binding selectivity
| Autor: | Philip M. Sher, Liesl G. Fisher, Steven M. Seiler, Inge M. Michel, S. Skwish, Gang Wu, Arvind Mathur, Kenneth E.J. Dickinson |
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| Rok vydání: | 1997 |
| Předmět: |
chemistry.chemical_classification
Agonist β3 adrenergic receptor Stereochemistry medicine.drug_class Organic Chemistry Clinical Biochemistry Pharmaceutical Science Sulfonic acid Biochemistry Chemical synthesis In vitro chemistry Drug Discovery medicine Molecular Medicine Adrenergic agonist Selectivity Molecular Biology Binding selectivity |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 7:1583-1588 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(97)00266-7 |
| Popis: | Carboxyl and other negatively charged groups were found to be most effective at producing human β3 adrenergic receptor binding selectivity in 1 (BRL 37344) and related compounds. The sulfonic acid analog 7 (BMS-187413) is a novel and potent β3 adrenergic agonist that binds selectively, and thus has an in vitro profile that compares favorably with that of BRL 37344. |
| Databáze: | OpenAIRE |
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