148729-69-5Relevant articles and documents
Novel benzimidazoles as ligands for the strychnine-insensitive N-methyl-D-aspartate-linked glycine receptor
Louvet, P.,Lallement, G.,Pernot-Marino, I.,Luu-Duc, C.,Blanchet, G.
, p. 71 - 75 (1993)
Two new benzimidazole derivatives were synthesized and evaluated for their ability to inhibit the binding at the strychnine-intensivite N-methyl-D-aspartate(NMDA)-linked glycine receptor.The most potent one, the 4,6-dichlorobenzimidazole-2-carboxylic acid
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: Potent human histamine H4 antagonists
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.
, p. 8289 - 8298 (2005)
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 H 4 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 initial pharmacokinetic studies were performed on selected compounds leading to the identification of indole 8 and benzimidazole 40 as potent H4 antagonists with the potential for further development. In addition, both 8 and 40 demonstrated efficacy in in vitro mast cell and eosinophil chemotaxis assays.
