New 1,2,4-oxadiazole derivatives: synthesis and adrenergic receptors binding studies

Farmaco. 1992 Jun;47(6):953-66.

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.

MeSH terms

  • Animals
  • Brain Chemistry / drug effects
  • In Vitro Techniques
  • Oxadiazoles / chemical synthesis*
  • Oxadiazoles / pharmacology
  • Rats
  • Receptors, Adrenergic / drug effects*
  • Receptors, Adrenergic, alpha / drug effects
  • Receptors, Adrenergic, alpha / metabolism
  • Receptors, Adrenergic, beta / drug effects
  • Receptors, Adrenergic, beta / metabolism

Substances

  • Oxadiazoles
  • Receptors, Adrenergic
  • Receptors, Adrenergic, alpha
  • Receptors, Adrenergic, beta