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

作者信息

Roy Caroline, Li Ticheao, Krasik Pavel, Gilbert Marie-Joseé, Pelletier Christine, Gagnon Diane, Robert Ed, Ducharme Julie, Storer Richard, Lavallée Jean-François

机构信息

Shire Biochem, 275 Armand-Frappier Blvd., Laval, H7V 4A7, Québec, Canada.

出版信息

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3141-3. doi: 10.1016/s0960-894x(02)00644-3.

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.