Bioorganic & Medicinal Chemistry Letters 2007-05-01

Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors.

Michael A Letavic, John M Keith, Kiev S Ly, Ann J Barbier, Jamin D Boggs, Sandy J Wilson, Brian Lord, Timothy W Lovenberg, Nicholas I Carruthers

Index: Bioorg. Med. Chem. Lett. 17(9) , 2566-9, (2007)

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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.