β1-Selective adrenoceptor antagonists. 2. 4-ether-linked

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

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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
Publication statusPublished - 1983
Externally publishedYes

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ASJC Scopus subject areas

  • Organic Chemistry

Cite this

Machin, P. J., Hurst, D. N., Bradshaw, R. M., Blaber, L. C., Burden, D. T., Fryer, A., ... Slivdasani, C. (1983). β1-Selective adrenoceptor antagonists. 2. 4-ether-linked. Journal of Medicinal Chemistry, 26(11), 1570-1576.