85613-37-2Relevant academic research and scientific papers
β1-Selective Adrenoceptor Antagonists: Examples of the 2-phenyl>imidazole Class. 2
Baldwin, John J.,Christy, Marcia E.,Denny, George H.,Habecker, Charles N.,Freedman, Mark B.,et al.
, p. 1065 - 1080 (2007/10/02)
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
β1-Selective adrenoceptor antagonists: Examples of the 2-[4-[3-(substituted-amino)-2-hydroxypropoxy]phenyl]imidazole class
Baldwin,Denny,Hirschmann,Freedman,Ponticello,Gross,Sweet
, p. 950 - 957 (2007/10/02)
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.
