β1-Selective Adrenoceptor Antagonists: Examples of the 2-phenyl>imidazole Class. 2
An attempt to develop a highly cardioselective β-adrenoceptor antagonist devoid of intrinsic sympathomimetic activity (ISA) focused on exploring structure-activity relationships around (S)--amino>-2-hydroxypropoxy>phen
Baldwin, John J.,Christy, Marcia E.,Denny, George H.,Habecker, Charles N.,Freedman, Mark B.,et al.
p. 1065 - 1080
(2007/10/02)
β1-Selective adrenoceptor antagonists: Examples of the 2-[4-[3-(substituted-amino)-2-hydroxypropoxy]phenyl]imidazole class
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.