Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine H4 antagonists

…, J Wei, PJ Desai, W Jiang, S Nguyen…

文献索引：Venable, Jennifer D.; Cai, Hui; Chai, Wenying; Dvorak, Curt A.; Grice, Cheryl A.; Jablonowski, Jill A.; Shah, Chandra R.; Kwok, Annette K.; Ly, Kiev S.; Pio, Barbara; Wei, Jianmei; Desai, Pragnya J.; Jiang, Wen; Nguyen, Steven; Ling, Ping; Wilson, Sandy J.; Dunford, Paul J.; Thurmond, Robin L.; Lovenberg, Timothy W.; Karlsson, Lars; Carruthers, Nicholas I.; Edwards, James P. Journal of Medicinal Chemistry, 2005 , vol. 48, # 26 p. 8289 - 8298

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被引用次数: 112

摘要

Three series of H4 receptor ligands, derived from indoly-2-yl-(4-methyl-piperazin-1-yl)- methanones, have been synthesized and their structure-activity relationships evaluated for activity at the H4 receptor in competitive binding and functional assays. In all cases, substitution of small lipophilic groups in the 4 and 5-positions led to increased activity in a [3H] histamine radiolabeled ligand competitive binding assay. In vitro metabolism and ...