European Journal of Medicinal Chemistry p. 743 - 755 (1995)
Update date:2022-08-03
Topics:
Balsamo
Breschi
Chiellini
Favero
Macchia
Martinelli
Martini
Rossello
Scatizzi
N-Isopropyl-(5a-g) and N-t-butyl-substituted (6a-g) (E)-N-[3-(amino)-2-hydroxypropylidene](arylmethyloxy)amines, which present an aromatic ring (Ar) linked to the CH2 carbon of the [(methyloxy)imino]methyl moiety (MOIMM), were synthesized with the aim of comparing their β-adrenergic properties with those of the previously studied completely aliphatic analogs 1,2 and 3,4. Compounds 5 and 6 were tested for their affinity towards β1- and β2-adrenoceptors by radioligand binding experiments; the compounds with the highest affinity were also assayed for their β1- and β2-adrenergic activity by functional tests on isolated preparations. The biopharmacological results show that, for the MOIM derivatives studied (1-6), the presence of an Ar substituent linked to the MOIM, as in 5 and 6, does not have any appreciable effect on the β1-adrenergic properties in terms of affinity and activity; this type of substituent, on the contrary, appears to be capable of improving the β2-adrenergic properties, as far as the receptor affinity is concerned. These results are discussed on the basis of a comparison of the conformational and electronic characteristics.
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