β1-Selective Adrenoceptor Antagonists. 2. 4-Ether-Linked Phenoxypropanolamines

Peter J. Machín, David N. Hurst, Rachel M. Bradshaw, Leslie C. Blaber, David T. Burden, Allison D. Fryer, Rosemary A. Melarange, Celia Shivdasani

Research output: Contribution to journalArticlepeer-review

13 Scopus citations

Abstract

A series of 4-substituted phenoxypropanolamines was prepared and examined for β-adrenoceptor activity. Some of the compounds, especially the [4-[2-[[2-(4-fluorophenyl)ethyl]oxy]ethoxy]phenoxy]propanolamines (14,15, and 24), showed potent β1-blockade with virtually no β2-blockade at doses over a 1000 times greater. The compounds also possessed partial agonist activity. Structure-activity relationships are discussed, and conclusions are drawn about the binding sites on β-adrenoceptors.

Original languageEnglish (US)
Pages (from-to)1570-1576
Number of pages7
JournalJournal of Medicinal Chemistry
Volume26
Issue number11
DOIs
StatePublished - Nov 1983
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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