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.

SYNTHESIS AND PHARMACOLOGICAL INVESTIGATION OF THE 3-ANALOGS OF VIMINOL

M. De Amici
Primo
;
C. De Micheli
Secondo
;
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.
adrenergic agents; analgesic agents; viminol analogs
Settore CHIM/08 - Chimica Farmaceutica
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2434/184384
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