Huang Charles Q, Wilcoxen Keith M, Grigoriadis Dimitri E, McCarthy James R, Chen Chen
Department of Medicinal Chemistry and Department of Pharmacology, Neurocrine Biosciences, Inc., 10555 Science Center Drive, San Diego, CA 92129, USA.
Bioorg Med Chem Lett. 2004 Aug 2;14(15):3943-7. doi: 10.1016/j.bmcl.2004.05.056.
A series of 3-(2-pyridyl)pyrazolo[1,5-a]pyrimidines was designed and synthesized as antagonists for the corticotrophin-releasing factor-1 (CRF(1)) receptor. Several compounds such as 20c (K(i)=10 nM) exhibited good binding affinities at the CRF(1) receptor. In addition, 20c had adequate solubility in water.
设计并合成了一系列3-(2-吡啶基)吡唑并[1,5-a]嘧啶作为促肾上腺皮质激素释放因子-1（CRF(1)）受体的拮抗剂。几种化合物，如20c（K(i)=10 nM）在CRF(1)受体上表现出良好的结合亲和力。此外，20c在水中具有足够的溶解度。
