Corpus ID: 20337042

Synthesis of new delta 2-isoxazoline derivatives and their pharmacological characterization as beta-adrenergic receptor antagonists.

@article{Conti1998SynthesisON,
  title={Synthesis of new delta 2-isoxazoline derivatives and their pharmacological characterization as beta-adrenergic receptor antagonists.},
  author={P. Conti and C. Dallanoce and M. De Amici and C. De Micheli and K. Klotz},
  journal={Bioorganic & medicinal chemistry},
  year={1998},
  volume={6 4},
  pages={
          401-8
        }
}
A series of delta 2-isoxazoline derivatives structurally related to Broxaterol 1 and Falintolol 3 has been prepared and evaluated for their binding affinity to beta 1- and beta 2-adrenergic receptors. Among the tested compounds only the 3-isopropenyl anti derivative 4d is as active as the reference compounds. An electron-releasing group, probably operating through a pi-pi interaction, in the 3-position of the isoxazoline nucleus greatly enhances the affinity of the compounds. Conversely, the… Expand
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