beta-Adrenergic blocking agents. 23. 1-[Substituted-amido)phenoxy]-3-[[(substituted-amido)alkyl]amino] propan-2-ols.
The synthesis of a series of 1-phenoxy-3-[(amidoalkyl)amino]propan-2-ols, in which the phenoxy ring is variously substituted with ortho and para amidic moieties, is described. Several of the compounds have beta-blocking potency comparable to that of propranolol and cardioselectivity similar to that of practolol, when given intravenously to anesthetized cats. In contrast to previous findings with cardioselective beta blockers, both ortho and para substitution give variable degrees of cardioselectivity. Potency, however, is favored by ortho substitution.
D000319:Adrenergic beta-Antagonists / Q000494:pharmacology*; D000818:Animals; D002415:Cats; D006321:Heart / Q000187:drug effects; D010647:Phenyl Ethers / Q000494:pharmacology*; D011217:Practolol / Q000494:pharmacology; D011412:Propanolamines / Q000494:pharmacology*; D011433:Propranolol / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000319:Adrenergic beta-Antagonists; D010647:Phenyl Ethers; D011412:Propanolamines; D011433:Propranolol; D011217:Practolol