Zusammenfassung
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 closest analogs of Broxaterol (3-bromo delta 2-isoxazolines
4a and 5a) are at least one order of magnitude less active than the
model compound 1. Throughout the series of derivatives the anti stereoisomers
are invariably more active than their syn counterparts.
Nutzer