2. Academic Validation
  3. Synthesis and structure-activity relationships of pyrazolo[1,5-a]pyridine derivatives: potent and orally active antagonists of corticotropin-releasing factor 1 receptor

Synthesis and structure-activity relationships of pyrazolo[1,5-a]pyridine derivatives: potent and orally active antagonists of corticotropin-releasing factor 1 receptor

  • J Med Chem. 2012 Jun 14;55(11):5255-69. doi: 10.1021/jm300259r.
Yoshinori Takahashi 1,  Shigeki Hibi,  Yorihisa Hoshino,  Koichi Kikuchi,  Kogyoku Shin,  Kaoru Murata-Tai,  Masae Fujisawa,  Mitsuhiro Ino,  Hisashi Shibata,  Masahiro Yonaga
Affiliations

Affiliation

  • 1 Medicinal Chemistry, Tsukuba Research Laboratories, Eisai Co., Ltd., 5-1-3 Tokodai, Tsukuba-shi, Ibaraki 300-2635, Japan. y4-takahashi@hhc.eisai.co.jp
PMID: 22587443 DOI: 10.1021/jm300259r
Abstract

Design, synthesis, and structure-activity relationships of a series of 3-dialkylamino-7-phenyl pyrazolo[1,5-a]pyridines (I) as selective antagonists of the corticotropin-releasing factor 1 (CRF(1)) receptor are described. The most prominent compound to emerge from this work, 46 (E2508), exhibits potent in vitro activity, excellent drug-like properties, and robust oral efficacy in animal models of stress-related disorders. It has advanced into clinical trials.

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