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The synthesis of a group of potential beta-blockers bearing a new 5-ethoxysalicylamide substituent on nitrogen is described. These compounds were tested for beta-adrenergic blocking potency in vitro and compared with analogous compounds bearing a tert-butyl group on nitrogen. The new N-substituent increased the beta-blocking potency substantially. In a series of five homologous compounds of the type Ar(CH2)nCHOHCH2NHR (R = 5-ethoxysalicylamide; n = 0-4), two maxima of beta-blocking potency were found for n = 0 and 2. Moreover, the carbon isostere of the corresponding (aryloxy)propanolamine still proved to be a very potent beta-blocker. The ether oxygen in the side chain is therefore not an absolute requirement for activity. Structure-activity relationships are discussed.
W Fuhrer, and
F Ostermayer, and
M Zimmermann, and
M Meier, and
H Müller
December 1969,
The Biochemical journal,
W Fuhrer, and
F Ostermayer, and
M Zimmermann, and
M Meier, and
H Müller
July 1983,
The Journal of pharmacology and experimental therapeutics,
W Fuhrer, and
F Ostermayer, and
M Zimmermann, and
M Meier, and
H Müller
January 1982,
Journal of emergency nursing,
W Fuhrer, and
F Ostermayer, and
M Zimmermann, and
M Meier, and
H Müller
September 1982,
Midwife, health visitor & community nurse,
W Fuhrer, and
F Ostermayer, and
M Zimmermann, and
M Meier, and
H Müller
March 1967,
The New England journal of medicine,
W Fuhrer, and
F Ostermayer, and
M Zimmermann, and
M Meier, and
H Müller
January 1967,
Duodecim; laaketieteellinen aikakauskirja,
W Fuhrer, and
F Ostermayer, and
M Zimmermann, and
M Meier, and
H Müller
May 1969,
Il Policlinico. Sezione pratica,
W Fuhrer, and
F Ostermayer, and
M Zimmermann, and
M Meier, and
H Müller
January 1971,
Journal of postgraduate medicine,
W Fuhrer, and
F Ostermayer, and
M Zimmermann, and
M Meier, and
H Müller
January 1976,
Progress in drug research. Fortschritte der Arzneimittelforschung. Progres des recherches pharmaceutiques,
W Fuhrer, and
F Ostermayer, and
M Zimmermann, and
M Meier, and
H Müller
January 1980,
Acta physiologica Academiae Scientiarum Hungaricae,
