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  • Title: New 1,2,4-oxadiazole derivatives: synthesis and adrenergic receptors binding studies.
    Author: Brizzi V, Brufani M, Filocamo L, Bruni G, Fiaschi AI.
    Journal: Farmaco; 1992 Jun; 47(6):953-66. PubMed ID: 1326978.
    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.
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