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

作者信息

Kam S T, Matier W L, Mai K X, Barcelon-Yang C, Borgman R J, O'Donnell J P, Stampfli H F, Sum C Y, Anderson W G, Gorczynski R J

出版信息

J Med Chem. 1984 Aug;27(8):1007-16. doi: 10.1021/jm00374a013.

Abstract

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.

摘要

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