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, 48 (16), 5104-7

Design and Synthesis of Tricyclic imidazo[4,5-b]pyridin-2-ones as Corticotropin-Releasing factor-1 Antagonists

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Design and Synthesis of Tricyclic imidazo[4,5-b]pyridin-2-ones as Corticotropin-Releasing factor-1 Antagonists

Zhiqiang Guo et al. J Med Chem.

Abstract

The synthesis and SAR studies of tricyclic imidazo[4,5-b]pyridin-2-ones as human corticotropin-releasing factor receptor (CRF(1)) antagonists are discussed herein. Compound 16g was identified as a functional antagonist that inhibited CRF-stimulated cyclic adenosine monophosphate production and CRF-induced adrenocorticotrophic hormone release. Pharmacokinetics studies in rats showed that 16g was orally bioavailable, had good brain penetration, and had a moderate half-life. In our effort to identify CRF(1) antagonists with improved pharmacokinetics properties, 16g exhibited a favorably lower volume of distribution.

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