Some selected stereoisomers of the 3-regioisomer of viminol 1 have been synthesized and studied as potential analgesic and adrenergic agents. In particular, we investigated those compounds possessing the (R,R) - or (S,S)-configuration at the di-sec. butylamine group and the R or S configuration at the secondary alcohol. The results indicate that compounds 2-5 did not possess the analgesic activity of viminol even if the (R,R)-isomers maintain a slight affinity towards opioid receptors. In addition, despite the presence of the ethanolamine moiety, none of the stereoisomers 2-5 exhibited an appreciable affinity for the adrenergic receptors.
SYNTHESIS AND PHARMACOLOGICAL INVESTIGATION OF THE 3-ANALOGS OF VIMINOL / M. De Amici, C. De Micheli, F. Platini, D. Della Bella, I. Caramazza. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - 23:6(1988), pp. 511-515. [10.1016/0223-5234(88)90093-1]
SYNTHESIS AND PHARMACOLOGICAL INVESTIGATION OF THE 3-ANALOGS OF VIMINOL
M. De AmiciPrimo
;C. De MicheliSecondo
;
1988
Abstract
Some selected stereoisomers of the 3-regioisomer of viminol 1 have been synthesized and studied as potential analgesic and adrenergic agents. In particular, we investigated those compounds possessing the (R,R) - or (S,S)-configuration at the di-sec. butylamine group and the R or S configuration at the secondary alcohol. The results indicate that compounds 2-5 did not possess the analgesic activity of viminol even if the (R,R)-isomers maintain a slight affinity towards opioid receptors. In addition, despite the presence of the ethanolamine moiety, none of the stereoisomers 2-5 exhibited an appreciable affinity for the adrenergic receptors.Pubblicazioni consigliate
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.