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 language||English (US)|
|Number of pages||7|
|Journal||Journal of Medicinal Chemistry|
|Publication status||Published - 1983|
ASJC Scopus subject areas
- Organic Chemistry