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
Discovery Chemistry-Wilmington, Bristol-Myers Squibb Company, Experimental Station, DE 19880, USA.
Bioorg Med Chem Lett. 2003 Jan 6;13(1):125-8. doi: 10.1016/s0960-894x(02)00833-8.
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 binding affinity are described herein.
