beta -Adrenergic blocking agents. 22. 1-Phenoxy-3(((substituted-amido)alkyl)amino)-2-propanols

The synthesis of a series of 1-phenoxy-3-(((substituted-amido)alkyl)amino)-2-propanols is described. Many of the compounds are more potent than propanolol as beta blockers, while having cardioselectivity comparable to that of practolol, when given intravenously to anesthetized cats. The structure-ac...

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Veröffentlicht in:Journal of medicinal chemistry 1982-01, Vol.25 (11), p.1286-1292
Hauptverfasser: Large, MS, Smith, L H
Format: Artikel
Sprache:eng
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Zusammenfassung:The synthesis of a series of 1-phenoxy-3-(((substituted-amido)alkyl)amino)-2-propanols is described. Many of the compounds are more potent than propanolol as beta blockers, while having cardioselectivity comparable to that of practolol, when given intravenously to anesthetized cats. The structure-activity relationships shown by this series of compounds provide further evidence that the addition of substituents to the alkylamino moeity of a beta blocker can confer cardioselectivity and that amidic substituents are remarkably effective.
ISSN:0022-2623