Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists

…, J Nelson, S Zamani-Kord, DE Grigoriadis…

文献索引：Gross, Raymond S.; Guo, Zhiqiang; Dyck, Brian; Coon, Tim; Huang, Charles Q.; Lowe, Richard F.; Marinkovic, Dragan; Moorjani, Manisha; Nelson, Jodene; Zamani-Kord, Said; Grigoriadis, Dimitri E.; Hoare, Sam R. J.; Crowe, Paul D.; Bu, Jane Han; Haddach, Mustapha; McCarthy, James; Saunders, John; Sullivan, Robert; Chen, TaKung; Williams, John P. Journal of Medicinal Chemistry, 2005 , vol. 48, # 18 p. 5780 - 5793

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被引用次数: 40

摘要

Antagonists of the corticotropin-releasing factor (CRF) neuropeptide should prove to be effective in treating stress and anxiety-related disorders. In an effort to identify antagonists with improved physicochemical properties, new tricyclic CRF1 antagonists were designed, synthesized, and tested for biological activity. As a result of studies aimed at establishing a relationship between structure and CRF1 binding affinity, NBI 35965 (12a) was identified ...