Potent, selective aminothiazolidinediones agonists of the human beta(3) adrenergic receptor

Citation
Ms. Malamas et al., Potent, selective aminothiazolidinediones agonists of the human beta(3) adrenergic receptor, MED CHEM RE, 10(3), 2000, pp. 164-177
Citations number
20
Categorie Soggetti
Chemistry & Analysis
Journal title
MEDICINAL CHEMISTRY RESEARCH
ISSN journal
10542523 → ACNP
Volume
10
Issue
3
Year of publication
2000
Pages
164 - 177
Database
ISI
SICI code
1054-2523(2000)10:3<164:PSAAOT>2.0.ZU;2-W
Abstract
A cloned human beta (3) adrenergic receptor assay was used to identify pote nt and selective beta (3) agonists. The thiazolidinedione moiety has been i dentified as a new pharmacophore for the human beta (3) adrenergic receptor . The versatility of the thiazolidinedione pharmacophore was demonstrated i n both the arylethanolamine and phenylpropanolamine families of beta (3) ag onists, where potent and selective compounds have been synthesized. Thiazol idinedione 20, a potent and selective human beta (3) agonist, increased the rmogenesis and lowered plasma glucose levels in the db/db mice.