John M Keith, Leslie A Gomez, Michael A Letavic, Kiev S Ly, Jill A Jablonowski, Mark Seierstad, Ann J Barbier, Sandy J Wilson, Jamin D Boggs, Ian C Fraser, Curt Mazur, Timothy W Lovenberg, Nicholas I Carruthers
A series of tetrahydroisoquinolines acting as dual histamine H3/serotonin transporter ligands is described. A highly regio-selective synthesis of the tetrahydroisoquinoline core involving acid mediated ring-closure of an acetophenone intermediate followed by reduction with NaCNBH3 was developed. In vitro and in vivo data are discussed.
February 1, 2007: Bioorganic & Medicinal Chemistry Letters