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

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...

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Bibliographic Details
Published in:	Journal of medicinal chemistry Vol. 27; no. 8; pp. 1007 - 1016
Main Authors:	Kam, Sheung Tsam, Matier, William L, Mai, Khuong X, Barcelon-Yang, Cynthia, Borgman, Robert J, O'Donnell, John P, Stampfli, Herman F, Sum, Check Y, Anderson, William G
Format:	Journal Article
Language:	English
Published:	United States American Chemical Society 01-08-1984
Subjects:	Adrenergic beta-Antagonists - chemical synthesis Adrenergic beta-Antagonists - pharmacology Animals Dogs Guinea Pigs Half-Life Heart Rate - drug effects Humans In Vitro Techniques Isoproterenol - pharmacology Propanolamines - chemical synthesis Propanolamines - pharmacology Structure-Activity Relationship Time Factors Trachea - drug effects
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Summary:	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.
Bibliography:	ark:/67375/TPS-RJ98NSD2-P istex:B1831C7DC388C962EF06CB7A367CFF32E534F431 ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00374a013