14539-67-4Relevant academic research and scientific papers
Synthesis and β-adrenergic activity of new completely aliphatic 3-(methyleneaminoxy)propanolamine derivatives
Balsamo,Gentili,Lapucci,Macchia,Martinelli,Orlandini,Ferni,Pinza
, p. 759 - 766 (2007/10/02)
In a previous paper, it had been found that completely aliphatic 3-(methyleneaminoxy)propanolamine derivatives showed a good β-blocking adrenergic activity directed prevalently towards β2-tracheal receptors. In an attempt to change the β-adrenergic properties of these compounds from antagonist to agonist, while still retaining the β2-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 β-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.
