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SYNTHESIS AND BETA-ADRENERGIC ACTIVITY OF NEW COMPLETELY ALIPHATIC 3-(METHYLENEAMINOXY)PROPANOLAMINE DERIVATIVES

Authors: BALSAMO A; GENTILI D; LAPUCCI, ANNALINA; MACCHIA, MARCO; MARTINELLI, ADRIANO; ORLANDINI, ELISABETTA;

SYNTHESIS AND BETA-ADRENERGIC ACTIVITY OF NEW COMPLETELY ALIPHATIC 3-(METHYLENEAMINOXY)PROPANOLAMINE DERIVATIVES

Abstract

In a previous paper, it had been found that completely aliphatic 3-(methylene aminoxy)propanolamine derivatives showed a good beta-blocking adrenergic activity directed prevalently towards beta(2)-tracheal receptors. In an attempt to change the beta-adrenergic properties of these compounds from antagonist to agonist, while still retaining the beta(2)-selectivity, a series of new completely aliphatic 3-(methyleneaminoxy)propanolamine derivatives were designed in which either a hydroxylic or a methoxylic group was present on the aliphatic portion linked to the oximic carbon. The synthesis of the new compounds and their beta-adrenergic activity, evaluated by means of functional tests on isolated preparations, are described and discussed; the results obtained are then rationalised on the basis of their conformational and reactivity characteristics, determined by means of theoretical methods.

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selected citations
These citations are derived from selected sources.
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
0
Average
Average
Average
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