Some totally aliphatic 3-(acyloxy)propanolamines were synthesized with the aim of testing whether @blocking activity could be obtained from this class of drugs, even in the absence of an aromatic group. The significant and, in most cases, competitive P-blocking activity shown by the compounds under examination, together with the results of a theoretical study in which their reactivity was compared with that of other adrenergic 0-blocking drugs, seems to confirm a hypothesis previously advanced on the basis of knowledge about the action mechanism of adrenergic P-blocking drugs and of the results of structural studies. It was also possible to suggest some considerations about the role played by the (acy1oxy)methyl portion of 3-(acyloxy)propanolamines in eliciting their adrenergic P-blocking activity.
|Autori interni:||LAPUCCI, ANNALINA|
BRESCHI, MARIA CRISTINA
|Autori:||MACCHIA B; BALSAMO A; LAPUCCI A; MACCHIA F; MARTINELLI A; AMMON H.L; PRASAD S. M; BRESCHI M.C; DUCCI M; MARTINOTTI E|
|Titolo:||ROLE OF THE (ACYLOXY)METHYL MOIETY IN ELICITING THE ADRENERGIC BETA-BLOCKING ACTIVITY OF 3-(ACYLOXY)PROPANOLAMINES|
|Anno del prodotto:||1987|
|Digital Object Identifier (DOI):||10.1021/jm00387a006|
|Appare nelle tipologie:||1.1 Articolo in rivista|