Publication | Closed Access
Cardioselective .beta.-adrenergic blocking agents. 1. 1-[(3,4-Dimethoxyphenethyl)amino]-3-aryloxy-2-propanols
54
Citations
0
References
1975
Year
Combinatorial ChemistryMolecular PharmacologyMedicinal ChemistryCardioselective Beta-blockadeOptimal PotencyMedicineMechanism Of ActionStructure-activity RelationshipsPharmacological AgentAnesthesiologyPharmacotherapyStereoselective SynthesisPharmacologyPharmaceutical ChemistryEnantioselective SynthesisDrug DiscoveryAlpha-adrenergic Pharmacology
A series of 1-amino-3-aryloxy-2-propanols has been synthesized and examined for cardioselective beta-blockade. The introduction of the (3,4-dimethoxyphenethyl)amino group lead to the most cardioselective agents. Structure-activity relationships are discussed. Of the compounds tested 1-[(3,4-dimethoxyphenethyl)amino]-3-(m-tolyloxy)-2-propanol was selected for clinical trial because of optimal potency and selectivity.