beta-Adrenergic blocking agents. 23. 1-[Substituted-amido)phenoxy]-3-[[(substituted-amido)alkyl]amino] propan-2-ols

The synthesis of a series of 1-phenoxy-3-[(amidoalkyl)amino]propan-2-ols, in which the phenoxy ring is variously substituted with ortho and para amidic moieties, is described. Several of the compounds have beta-blocking potency comparable to that of propranolol and cardioselectivity similar to that...

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Bibliographic Details
Published inJournal of medicinal chemistry Vol. 26; no. 3; pp. 352 - 357
Main Authors Large, M S, Smith, L H
Format Journal Article
LanguageEnglish
Published United States 01.03.1983
Subjects
Adrenergic beta-Antagonists - pharmacology
Animals
Cats
Heart - drug effects
Phenyl Ethers - pharmacology
Practolol - pharmacology
Propanolamines - pharmacology
Propranolol - pharmacology
Structure-Activity Relationship
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Summary:The synthesis of a series of 1-phenoxy-3-[(amidoalkyl)amino]propan-2-ols, in which the phenoxy ring is variously substituted with ortho and para amidic moieties, is described. Several of the compounds have beta-blocking potency comparable to that of propranolol and cardioselectivity similar to that of practolol, when given intravenously to anesthetized cats. In contrast to previous findings with cardioselective beta blockers, both ortho and para substitution give variable degrees of cardioselectivity. Potency, however, is favored by ortho substitution.
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SourceType-Scholarly Journals-1
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content type line 23
ISSN:0022-2623
DOI:10.1021/jm00357a008