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