Imidazo [4, 5-b] pyridines as corticotropin releasing factor receptor ligands

…, CA Teleha, LW Fitzgerald, J McElroy, R Zaczek…

文献索引：Arvanitis, Argyrios G; Rescinito, Joseph T; Arnold, Charles R; Wilde, Richard G; Cain, Gary A; Sun, Jung Hui; Yan, Jia-Sheng; Teleha, Christopher A; Fitzgerald, Lawrence W; McElroy, John; Zaczek, Robert; Hartig, Paul R; Grossman, Scott; Arneric, Stephen P; Gilligan, Paul J; Olson, Richard E; Robertson, David W Bioorganic and medicinal chemistry letters, 2003 , vol. 13, # 1 p. 125 - 128

全文：HTML全文

被引用次数: 20

摘要

A series of high affinity CRF receptor ligands with an imidazo [4, 5-b] pyridine core is described. Individual analogues were synthesized and tested in a rat CRF receptor binding assay. The best compounds were further tested in the dog N-in-1 pharmacokinetic model to assess plasma levels at 1mg/kg (po) and in the rat situational anxiety model to assess anxiolytic efficacy at 3mg/kg (po). The structure–activity relationships for good receptor ...