Dual serotonin transporter/histamine H 3 ligands: optimization of the H 3 pharmacophore

…, KS Ly, JA Jablonowski, M Seierstad, AJ Barbier…

文献索引：Keith, John M.; Gomez, Leslie A.; Letavic, Michael A.; Ly, Kiev S.; Jablonowski, Jill A.; Seierstad, Mark; Barbier, Ann J.; Wilson, Sandy J.; Boggs, Jamin D.; Fraser, Ian C.; Mazur, Curt; Lovenberg, Timothy W.; Carruthers, Nicholas I. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 3 p. 702 - 706 Title/Abstract Full Text View citing articles Show Details Letavic, Michael A.; Keith, John M.; Jablonowski, Jill A.; Stocking, Emily M.; Gomez, Leslie A.; Ly, Kiev S.; Miller, Jennifer M.; Barbier, Ann J.; Bonaventure, Pascal; Boggs, Jamin D.; Wilson, Sandy J.; Miller, Kirsten L.; Lord, Brian; McAllister, Heather M.; Tognarelli; Wu, Jiejun; Abad, Marta C.; Schubert, Carsten; Lovenberg, Timothy W.; Carruthers, Nicholas I. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 4 p. 1047 - 1051

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被引用次数: 33

摘要

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.