title: Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors.
abstract: A series of novel tetrahydronaphthyridine-based histamine H(3) ligands that have serotonin reuptake transporter inhibitor activity is described. The 1,2,3,4-tetrahydro-2,6-naphthyridine scaffold is assembled via the addition of a nitrostyrene to a metalated pyridine followed by reduction and cyclization to form the naphthyridine. In vitro biological data for these novel compounds are discussed.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121-1126, USA. mletavic@prdus.jnj.com
authors.forename: Michael A
authors.initials: MA
authors.lastname: Letavic
authors.forename: John M
authors.initials: JM
authors.lastname: Keith
authors.forename: Kiev S
authors.initials: KS
authors.lastname: Ly
authors.forename: Ann J
authors.initials: AJ
authors.lastname: Barbier
authors.forename: Jamin D
authors.initials: JD
authors.lastname: Boggs
authors.forename: Sandy J
authors.initials: SJ
authors.lastname: Wilson
authors.forename: Brian
authors.initials: B
authors.lastname: Lord
authors.forename: Timothy W
authors.initials: TW
authors.lastname: Lovenberg
authors.forename: Nicholas I
authors.initials: NI
authors.lastname: Carruthers
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D006632:Histamine / Q000737:chemistry*; D006633:Histamine Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D008956:Models, Chemical; D008968:Molecular Conformation; D009287:Naphthyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D018100:Receptors, Histamine H3 / Q000737:chemistry*; D012701:Serotonin / Q000378:metabolism; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D006632:Histamine; D006633:Histamine Antagonists; D009287:Naphthyridines; D018100:Receptors, Histamine H3; D012701:Serotonin; D017367:Selective Serotonin Reuptake Inhibitors