5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists

…, PM Andrae, J Mattes, J Zhang, A Kramer…

文献索引：Haydar, Simon N.; Yun, Heedong; Andrae, Patrick M.; Mattes, James; Zhang, Jean; Kramer, Angela; Smith, Deborah L.; Huselton, Christine; Graf, Radka; Aschmies, Suzan; Schechter, Lee E.; Comery, Thomas A.; Robichaud, Albert J. Journal of Medicinal Chemistry, 2010 , vol. 53, # 6 p. 2521 - 2527

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被引用次数: 8

摘要

Novel 5-cyclic amine-3-arylsulfonylindazoles were prepared, and several analogues within this class have been identified as high-affinity 5-HT6 receptor ligands with improved pharmacokinetic and pharmacological properties. One selected example, 18b, showed good brain penetrability and a generally favorable pharmacokinetic profile with procognitive efficacy in the rat novel object recognition assay. The synthesis and structure− activity ...