[(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action.

Autor: Kam ST, Matier WL, Mai KX, Barcelon-Yang C, Borgman RJ, O'Donnell JP, Stampfli HF, Sum CY, Anderson WG, Gorczynski RJ, et. al.
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 1984 Aug; Vol. 27 (8), pp. 1007-16.
DOI: 10.1021/jm00374a013
Abstrakt: Novel [(arylcarbonyl)oxy]propanolamines were synthesized and investigated as potential ultrashort-acting beta-adrenergic receptor blockers. Many of these analogues exhibited good potency and short duration. The N-ureidoalkyl analogue 85 (ACC-9089) has a potency equal to propranolol and a duration of action of about 21 min in the dog. It has been selected as a candidate for further clinical study. Structure-activity relationships and structure-duration relationships for these new beta-blockers are also discussed.
Databáze: MEDLINE