Synthesis and pharmacological evaluation of new compounds with a potential action on the adrenergic system.
A series of compounds with a potential activity on both alpha and beta-adrenoreceptors were synthesized and evaluated with in vitro and in vivo tests. Aryloxypropanolamino derivatives N-substituted with alpha 2-benzodioxanylmethyl group showed a favourable alpha/beta ratio and a high selectivity towards beta 1 receptors. Substitution with different aralkyl groups afforded compounds with a low alpha-activity, although with a high potency and selectivity towards beta 1 receptors. The results are discussed on the basis of the working hypothesis and compared with those obtained for reference compounds.
D000317:Adrenergic alpha-Antagonists / Q000138:chemical synthesis*; D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis*; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D009119:Muscle Contraction / Q000187:drug effects; D011817:Rabbits; D013329:Structure-Activity Relationship
D000317:Adrenergic alpha-Antagonists; D000319:Adrenergic beta-Antagonists