Synthesis and pharmacological evaluation of propranolol-cyclic analogues.
Three propranolol analogues, bearing the oxygen of the --OH group enclosed in a 1,4-dioxanic rigid system, were synthetized. The lack of beta-blocking activity found for these compounds demonstrates the important role played by a free--OH group in the drug-receptor interaction.
D000317:Adrenergic alpha-Antagonists / Q000138:chemical synthesis; D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis; D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D011433:Propranolol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D014961:X-Ray Diffraction
D000317:Adrenergic alpha-Antagonists; D000319:Adrenergic beta-Antagonists; D011433:Propranolol