Details

Autor(en) / Beteiligte

• Keith, John M.
• Gomez, Leslie A.
• Wolin, Ronald L.
• Barbier, Ann J.
• Wilson, Sandy J.
• Boggs, Jamin D.
• Mazur, Curt
• Fraser, Ian C.
• Lord, Brian
• Aluisio, Leah
• Lovenberg, Timothy W.
• Carruthers, Nicholas I.

Titel

Pyrrolidino-tetrahydroisoquinolines as potent dual H 3 antagonist and serotonin transporter inhibitors

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2007-05, Vol.17 (9), p.2603-2607

Ort / Verlag

Elsevier Ltd

Erscheinungsjahr

2007

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• A series of novel and potent pyrrolidino-tetrahydroisoquinolines with dual histamine H 3 antagonist/serotonin transporter inhibitor activity is described. A highly regio- and diastereoselective synthesis of the pyrrolidino-tetrahydroisoquinoline core involving acid mediated ring-closure of an acetophenone intermediate followed by reduction with NaCNBH 3 was developed. In vitro and in vivo data are discussed. A series of novel and potent pyrrolidino-tetrahydroisoquinolines with dual histamine H 3 antagonist/serotonin transporter inhibitor activity is described. A highly regio- and diastereoselective synthesis of the pyrrolidino-tetrahydroisoquinoline core involving acid mediated ring-closure of an acetophenone intermediate followed by reduction with NaCNBH 3 was developed. In vitro and in vivo data are discussed.