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

…, I Sugimoto, T Matsushita, T Nishiyama, T Hirota…

文献索引：Saito, Tetsuji; Obitsu, Tetsuo; Kohno, Hiroshi; Sugimoto, Isamu; Matsushita, Takeshi; Nishiyama, Taihei; Hirota, Tomoko; Takeda, Hiroyuki; Matsumura, Naoya; Ueno, Sonoko; Kishi, Akihiro; Kagamiishi, Yoshifumi; Nakai, Hisao; Takaoka, Yoshikazu Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 2 p. 1122 - 1138

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被引用次数: 9

摘要

To identify structurally novel corticotropin-releasing factor 1 (CRF1) 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 ...