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;
1982-01-01
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.File in questo prodotto:
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