The two diastereoisomeric 3-(p-nitrophenyl)-6-methyl-3-piperidinols, which can be viewed as cyclic analogs of INPEA, were prepd. and pharmacol. examd. Their configurations and conformations were established by 1H NMR spectroscopy and IR studies in dil. soln. A pharmacol. assay of the above compds. for their competitive antagonism showed that the cis diastereoisomer, but not the trans, maintains the ability to interact with the β-adrenoceptor, although, compared to INPEA, the potency is reduced.
|Autori:||BALSAMO A; BARILI P.L; GAGLIARDI M; LAPUCCI A; MACCHIA B; MACCHIA F; BERGAMASCHI M|
|Titolo:||Synthesis and adrenergic beta-blocking activity of diastereoisomeric 3-(p-nitrophenyl)-6-methyl-3-piperidinols|
|Anno del prodotto:||1982|
|Appare nelle tipologie:||1.1 Articolo in rivista|