Dual serotonin transporter inhibitor/histamine H 3 antagonists: Development of rigidified H 3 pharmacophores
…, JD Boggs, IC Fraser, C Mazur, TW Lovenberg…
文献索引：Keith, John M.; Barbier, Ann J.; Wilson, Sandy J.; Miller, Kirstin; Boggs, Jamin D.; Fraser, Ian C.; Mazur, Curt; Lovenberg, Timothy W.; Carruthers, Nicholas I. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 19 p. 5325 - 5329
A series of tetrahydroisoquinolines acting as dual serotonin transporter inhibitor/histamine H3 antagonists is described. The introduction of polar aromatic spacers as part of the histamine H3 pharmacophore was explored. A convergent synthesis of the final products allowing late stage introduction of the aromatic side chain was developed. In vitro and in vivo data are discussed.
