Journal of Medicinal Chemistry p. 831 - 836 (1984)
Update date:2022-07-30
Topics:
Fuhrer
Ostermayer
Zimmermann
Meier
Mueller
The synthesis of a group of potential β-blockers bearing a new 5-ethoxysalicylamide substituent on nitrogen is described. These compounds were tested for β-adrenergic blocking potency in vitro and compared with analogous compounds bearing a tert-butyl group on nitrogen. The new N-substituent increased the β-blocking potency substantially. In a series of five homologous compounds of the type Ar(CH2)(n)CHOHCH2NHR (R = 5-ethoxysalicylamide; n = 0-4), two maxima of β-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 β-blocker. The ether oxygen in the side chain is therefore not an absolute requirement for activity. Structure-activity relationships are discussed.
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