Ontology highlight
ABSTRACT:
SUBMITTER: Mistry SN
PROVIDER: S-EPMC3694353 | biostudies-literature | 2013 May
REPOSITORIES: biostudies-literature
Mistry Shailesh N SN Baker Jillian G JG Fischer Peter M PM Hill Stephen J SJ Gardiner Sheila M SM Kellam Barrie B
Journal of medicinal chemistry 20130510 10
β-Adrenoceptor antagonists boast a 50-year use for symptomatic control in numerous cardiovascular diseases. One might expect highly selective antagonists are available for the human β-adrenoceptor subtype involved in these diseases, yet few truly β1-selective molecules exist. To address this clinical need, we re-evaluated LK 204-545 (1), (1) a selective β1-adrenoceptor antagonist, and discovered it possessed significant partial agonism. Removal of 1's aromatic nitrile afforded 19, a ligand with ...[more]