β1-Selective adrenoceptor antagonists: Examples of the 2-[4-[3-(substituted-amino)-2-hydroxypropoxy]phenyl]imidazole class

Article abstract of DOI:10.1021/jm00361a004

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.