新型萘啶类化合物是组胺H3拮抗剂和5-羟色胺再摄取转运体抑制剂。
Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors.
作者信息
Letavic Michael A, Keith John M, Ly Kiev S, Barbier Ann J, Boggs Jamin D, Wilson Sandy J, Lord Brian, Lovenberg Timothy W, Carruthers Nicholas I
机构信息
Johnson & Johnson Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121-1126, USA.
出版信息
Bioorg Med Chem Lett. 2007 May 1;17(9):2566-9. doi: 10.1016/j.bmcl.2007.02.006. Epub 2007 Feb 4.
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.
描述了一系列具有5-羟色胺再摄取转运体抑制剂活性的基于四氢萘啶的新型组胺H(3)配体。1,2,3,4-四氢-2,6-萘啶骨架是通过将硝基苯乙烯加成到金属化吡啶上，然后还原和环化以形成萘啶来构建的。讨论了这些新型化合物的体外生物学数据。
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