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

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
13
Issue
1
Identifiers
DOI: 10.1016/s0960-894x(02)00833-8
Disciplines
  • Pharmacology

Abstract

Abstract 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 1 mg/kg (po) and in the rat situational anxiety model to assess anxiolytic efficacy at 3 mg/kg (po). The structure–activity relationships for good receptor binding affinity are described herein.

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