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Bioorg Med Chem. 2012 Jan 15;20(2):1122-38. doi: 10.1016/j.bmc.2011.11.015. Epub 2011 Dec 3.

Pyrrolo[1,2-b]pyridazines, pyrrolo[2,1-f]triazin-4(3H)-ones, and related compounds as novel corticotropin-releasing factor 1 (CRF₁) receptor antagonists.

Author information

1
Minase Research Institute, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima, Osaka 618-8585, Japan. te.saitou@ono.co.jp

Abstract

To identify structurally novel corticotropin-releasing factor 1 (CRF(1)) receptor antagonists, a series of bicyclic core analogs pyrrolo[1,2-b]pyridazines and pyrrolo[2,1-f]triazin-4(3H)-ones, which were designed based on a monocyclic core antagonist, was synthesized and evaluated. Among the compounds tested, 2-difluoromethoxy-4-methylpyridin-5-yl analog 27 was found to show efficacy in a dose-dependent manner in an elevated plus maze test in rats. The discovery process and structure-activity relationship is presented.

PMID:
22196514
DOI:
10.1016/j.bmc.2011.11.015
[Indexed for MEDLINE]

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