67655-19-0Relevant articles and documents
β1-Selective Adrenoceptor Antagonists. 1. Synthesis and β-Adrenergic Blocking Activity of a Series of Binary (Aryloxy)propanolamines
Kierstead, R. W.,Faraone, A.,Mennona, F.,Mullin, J.,Guthrie, R. W.,et al.
, p. 1561 - 1569 (2007/10/02)
A series of binary (aryloxy)propanolamines has been prepared and examined in vitro and in vivo for β-adrenoreceptor blocking activity.These symmetrical compounds consist of two (S)-(phenyloxy)propanolamine pharmacophores coupled through alkylenedioxy or poly(oxyethylenedioxy) linking units of varying lengths.Examples of such binary compounds linked through the 2,2', 3,3', and 4,4' positions in the aromatic rings of the pharmacophores have been prepared.In vitro and in vivo test data indicate that the 2,2' compounds tend to be selective β2-adrenergic blocking agents, the 4,4' binaries tend to be selective β1-blocking agents, and those compounds with 3,3' linkages exhibit intermediate selectivities.One of the 4,4'-linked binary compounds, 4s, exhibited potent, cardioselective β-blockade in vivo, which was of short duration and was accompanied by a prolonged tachycardia.
