Synthesis and structure--activity relationship of novel aminotetralin derivatives with high micro selective opioid affinity

Several novel racemic aminotetralin derivatives have been prepared using a stereoselective aziridine ring opening reactions and were evaluated for their micro-opioid receptor binding affinity. Selectivity index towards other opioid receptors and antinociceptive activity in mice have been evaluated f...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2002-11, Vol.12 (21), p.3141-3143
Hauptverfasser:	Roy, Caroline, Li, Ticheao, Krasik, Pavel, Gilbert, Marie-Joseé, Pelletier, Christine, Gagnon, Diane, Robert, Ed, Ducharme, Julie, Storer, Richard, Lavallée, Jean-François
Format:	Artikel
Sprache:	eng
Schlagworte:	Analgesics, Opioid - chemical synthesis Analgesics, Opioid - pharmacology Animals Indicators and Reagents Mice Pain Measurement - drug effects Receptors, Opioid, delta - drug effects Receptors, Opioid, delta - metabolism Receptors, Opioid, kappa - drug effects Receptors, Opioid, kappa - metabolism Receptors, Opioid, mu - drug effects Stereoisomerism Structure-Activity Relationship Tetrahydronaphthalenes - chemical synthesis Tetrahydronaphthalenes - pharmacology
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Zusammenfassung:	Several novel racemic aminotetralin derivatives have been prepared using a stereoselective aziridine ring opening reactions and were evaluated for their micro-opioid receptor binding affinity. Selectivity index towards other opioid receptors and antinociceptive activity in mice have been evaluated for the most potent derivatives.
ISSN:	0960-894X