Synthesis and structure–activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor

…, T Furuuchi, M Yamauchi, F Yokoyama, N Kakui…

文献索引：Ishikawa, Makoto; Furuuchi, Takeshi; Yamauchi, Miki; Yokoyama, Fumikazu; Kakui, Nobukazu; Sato, Yasuo Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 14 p. 5441 - 5448

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被引用次数: 10

摘要

4-((1H-Imidazol-4-yl) methyl)-1-aryl-piperazine and piperidine derivatives were designed and synthesized as candidate human histamine type 3 agonists. The piperazine derivatives were found to have low (or no) affinity for human histamine H3 receptor, whereas the piperidine derivatives showed moderate to high affinity, and their agonistic activity was greatly influenced by substituents on the aromatic ring. Among the piperidine-containing ...