Pyrazolo [1, 5-a] pyrimidines, triazolo [1, 5-a] pyrimidines and their tricyclic derivatives as corticotropin-releasing factor 1 (CRF 1) receptor antagonists

…, T Obitsu, C Minamoto, T Sugiura, N Matsumura…

Index: Saito, Tetsuji; Obitsu, Tetsuo; Minamoto, Chiaki; Sugiura, Tsuneyuki; Matsumura, Naoya; Ueno, Sonoko; Kishi, Akihiro; Katsumata, Seishi; Nakai, Hisao; Toda, Masaaki Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 20 p. 5955 - 5966

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Citation Number: 21

Abstract

To identify structurally novel CRF1 receptor antagonists, a series of bicyclic core antagonists, pyrazolo [1, 5-a] pyrimidines, triazolo [1, 5-a] pyrimidines, imidazo [1, 2-a] pyrimidines and pyrazolo [1, 5-a][1, 3, 5] triazines were designed, synthesized and evaluated as CRF1 receptor antagonists. Compounds 2–27 showed binding affinity (IC50= 4.2–418nM) and antagonist activity (EC50= 4.0–889nM). Compound 5 was found to show ...