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.
ROLE OF THE (ACYLOXY)METHYL MOIETY IN ELICITING THE ADRENERGIC BETA-BLOCKING ACTIVITY OF 3-(ACYLOXY)PROPANOLAMINES
LAPUCCI, ANNALINA;MARTINELLI, ADRIANO;BRESCHI, MARIA CRISTINA;DUCCI, MICHELE;
1987-01-01
Abstract
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
