title: New 1,2,4-oxadiazole derivatives: synthesis and adrenergic receptors binding studies.
abstract: In order to obtain derivatives with simultaneous alpha- and beta-adrenergic blocking activity, compounds having the phenoxypropanolaminic structure of beta-adrenergic blockers have been synthesised, as well as 1,2,4-oxadiazole moiety, which could imitate the imidazolinic nucleus characteristic of drugs acting on alpha-adrenergic receptors. The synthesised compounds have been submitted to alpha and beta receptor binding assays. Some derivatives showed an alpha-adrenoceptor binding activity higher than labetalol and similar to prazosin, but with a poor beta-adrenoceptor binding activity.
authors.affiliation: Dipartmento Farmaco-Chimico-Tecnologico, Università Di Siena.
authors.forename: V
authors.initials: V
authors.lastname: Brizzi
authors.forename: M
authors.initials: M
authors.lastname: Brufani
authors.forename: L
authors.initials: L
authors.lastname: Filocamo
authors.forename: G
authors.initials: G
authors.lastname: Bruni
authors.forename: A I
authors.initials: AI
authors.lastname: Fiaschi
mesh_terms: D000818:Animals; D001923:Brain Chemistry / Q000187:drug effects; D066298:In Vitro Techniques; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011941:Receptors, Adrenergic / Q000187:drug effects*; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects / Q000378:metabolism; D011943:Receptors, Adrenergic, beta / Q000187:drug effects / Q000378:metabolism
chemical_list: D010069:Oxadiazoles; D011941:Receptors, Adrenergic; D011942:Receptors, Adrenergic, alpha; D011943:Receptors, Adrenergic, beta