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.

Synthesis and adrenergic beta-blocking activity of diastereoisomeric 3-(p-nitrophenyl)-6-methyl-3-piperidinols

LAPUCCI, ANNALINA;
1982

Abstract

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.
Balsamo, A; BARILI P., L; Gagliardi, M; Lapucci, Annalina; Macchia, B; Macchia, F; Bergamaschi, M.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11568/205637
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