New oxadiazolidinedione derivatives as potent and selective human beta3 agonists
| Autor: | John W. Ellingboe, Ruth Mulvey, Stella Han, Elwood Largis, Michael S. Malamas, Baihua Hu, Jeff Tillett |
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| Rok vydání: | 2001 |
| Předmět: |
Agonist
Adrenergic receptor Stereochemistry medicine.drug_class Clinical Biochemistry Pharmaceutical Science Adrenergic beta-3 Receptor Agonists CHO Cells Biochemistry Chemical synthesis Sensitivity and Specificity Structure-Activity Relationship Cricetinae Drug Discovery medicine Cyclic AMP Animals Humans Thiazolidinedione Receptor Molecular Biology Oxadiazoles Chemistry Organic Chemistry Biological activity Adrenergic beta-Agonists In vitro Thiazoles Molecular Medicine Thiazolidinediones Selectivity Protein Binding |
| Zdroj: | Bioorganicmedicinal chemistry letters. 11(8) |
| ISSN: | 0960-894X |
| Popis: | As part of our investigation into the development of potent and selective human β 3 agonists, a series of thiazolidinedione analogues was prepared and evaluated for their biological activity on the human β 3 -adrenergic receptor. The oxadiazolidinedione derivative 17 was found to be the most potent and selective compound in this study, with an EC 50 value of 0.02 μM at the β 3 receptor, 259-fold selectivity over the β 1 receptor, and 745-fold selectivity over the β 2 receptor. |
| Databáze: | OpenAIRE |
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