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A series of binary (aryloxy)propanolamines has been prepared and examined in vitro and in vivo for beta-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 beta 2-adrenergic blocking agents, the 4,4' binaries tend to be selective beta 1-blocking agents, and those compounds with 3,3' linkages exhibit intermediate selectivities. One of the 4,4'-linked binary compounds, 4s, exhibited potent, cardioselective beta-blockade in vivo, which was of short duration and was accompanied by a prolonged tachycardia.
R W Kierstead, and
A Faraone, and
F Mennona, and
J Mullin, and
R W Guthrie, and
H Crowley, and
B Simko, and
L C Blaber
June 1984,
Journal of medicinal chemistry,
R W Kierstead, and
A Faraone, and
F Mennona, and
J Mullin, and
R W Guthrie, and
H Crowley, and
B Simko, and
L C Blaber
October 1981,
Journal of medicinal chemistry,
R W Kierstead, and
A Faraone, and
F Mennona, and
J Mullin, and
R W Guthrie, and
H Crowley, and
B Simko, and
L C Blaber
December 1982,
Journal of medicinal chemistry,
R W Kierstead, and
A Faraone, and
F Mennona, and
J Mullin, and
R W Guthrie, and
H Crowley, and
B Simko, and
L C Blaber
June 1993,
Drug design and discovery,
R W Kierstead, and
A Faraone, and
F Mennona, and
J Mullin, and
R W Guthrie, and
H Crowley, and
B Simko, and
L C Blaber
January 1993,
Journal of medicinal chemistry,
R W Kierstead, and
A Faraone, and
F Mennona, and
J Mullin, and
R W Guthrie, and
H Crowley, and
B Simko, and
L C Blaber
April 1986,
Archivos de farmacologia y toxicologia,
R W Kierstead, and
A Faraone, and
F Mennona, and
J Mullin, and
R W Guthrie, and
H Crowley, and
B Simko, and
L C Blaber
December 1982,
Journal of medicinal chemistry,
R W Kierstead, and
A Faraone, and
F Mennona, and
J Mullin, and
R W Guthrie, and
H Crowley, and
B Simko, and
L C Blaber
April 1995,
Farmaco (Societa chimica italiana : 1989),
R W Kierstead, and
A Faraone, and
F Mennona, and
J Mullin, and
R W Guthrie, and
H Crowley, and
B Simko, and
L C Blaber
May 1987,
Journal of medicinal chemistry,
R W Kierstead, and
A Faraone, and
F Mennona, and
J Mullin, and
R W Guthrie, and
H Crowley, and
B Simko, and
L C Blaber
December 1991,
Drug design and discovery,
