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

Argyrios G. Arvanitis,Joseph T. Rescinito,Charles R. Arnold,Richard G. Wilde,Lawrence W. Fitzgerald,Robert Zaczek,Paul R. Hartig,Scott Grossman,Stephen P. Arneric,Paul J. Gilligan,Richard E. Olson,David W. Robertson

Bioorganic & Medicinal Chemistry Letters（2003）

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摘要

A series of high affinity CRF receptor ligands with an imidazo[4,5-c]pyridine core is described. Individual analogues were synthesized and tested in vitro in rat brain receptors to determine binding affinity. The best compound was further tested in the dog N-in-1 pharmacokinetic model to assess oral bioavailability at 1 mg/kg po.

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structure activity relationship

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