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. published their research in Journal of Medicinal Chemistry on December 29 ,2005. The article was titled 《Preparation and Biological Evaluation of Indole, Benzimidazole, and Thienopyrrole Piperazine Carboxamides: Potent Human Histamine H4 Antagonists》.Product Details of 3584-66-5 The article contains the following contents:
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 initial pharmacokinetic studies were performed on selected compounds leading to the identification of carboxamides I [X = CH, N] as potent H4 antagonists with the potential for further development. In addition, I demonstrated efficacy in in vitro mast cell and eosinophil chemotaxis assays. After reading the article, we found that the author used 5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole(cas: 3584-66-5Product Details of 3584-66-5)
5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole(cas: 3584-66-5) belongs to imidazoles.Imidazole rings are part of unnatural cyclic peptides and are used as ester isosteres in peptidomimetic studies.
However, the application of imidazoles is not limited to the field of peptides and peptidomimetics. Product Details of 3584-66-5
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem