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Synthesis and structure--activity relationship of novel aminotetralin derivatives with high micro selective opioid
Caroline Roy1, Ticheao Li, Pavel Krasik
1Shire Biochem, 275 Armand-Frappier Blvd., Laval, H7V 4A7, Québec, Canada. croy@ca.shire.com
Bioorganic & Medicinal Chemistry Letters
|October 10, 2002
Abstract:
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.