Discovery of pyrrolo [2, 3-d] pyrimidin-4-ones as corticotropin-releasing factor 1 receptor antagonists with a carbonyl-based hydrogen bonding acceptor

…, K Kobayashi, M Mochizuki, N Kanzaki, Y Sako…

文献索引：Aso, Kazuyoshi; Kobayashi, Katsumi; Mochizuki, Michiyo; Kanzaki, Naoyuki; Sako, Yuu; Yano, Takahiko Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 8 p. 2365 - 2371

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被引用次数: 6

摘要

A new class of pyrrolo [2, 3-d] pyrimidin-4-one corticotropin-releasing factor 1 (CRF1) receptor antagonists has been designed and synthesized. In general, reported CRF1 receptor antagonists possess a sp2-nitrogen atom as hydrogen bonding acceptor (HBA) on their core scaffolds. We proposed to use a carbonyl group of pyrrolo [2, 3-d] pyrimidin-4-one derivatives as a replacement for the sp2-nitrogen atom as HBA in classical CRF1 receptor ...