Journal of Medicinal Chemistry p. 950 - 957 (1983)
Update date:2022-08-03
Topics:
Baldwin
Denny
Hirschmann
Freedman
Ponticello
Gross
Sweet
A series of 2-[4-[3-(substituted-amino)-2-hydroxypropoxy]phenyl]imidazoles is described. The compounds were investigated in vitro for β-adrenoceptor antagonism, and several examples were found to be selective for the β1-adrenoceptor. The structure-activity relationship exhibited by this series of compounds is discussed. (S)-2-[p-[3-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-2-hydroxypropoxy]phenyl] -4-(2-thienyl)imidazole [(S)-13] was over 100 times more selective than atenolol for the β1-adrenergic receptor and has been selected for in-depth studies.
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