Yoon, Taeyoung ; Lombaert, Stephane De ; Brodbeck, Robbin ; Gulianello, Michael ; Krause, James E. ; Hutchison, Alan ; Horvath, Raymond F. ; Ge, Ping ; Kehne, John ; Hoffman, Diane ; Chandrasekhar, Jayaraman ; Doller, Dario ; Hodgetts, Kevin J. (2008) 2-Arylpyrimidines: novel CRF-1 receptor antagonists Bioorganic & Medicinal Chemistry Letters, 18 (16). pp. 4486-4490. ISSN 0960-894X
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Official URL: http://linkinghub.elsevier.com/retrieve/pii/S09608...
Related URL: http://dx.doi.org/10.1016/j.bmcl.2008.07.063
Abstract
The design, synthesis and structure-activity relationship studies of a novel series of CRF-1 receptor antagonists, the 2-arylpyrimidines, are described. The effects of substitution on the aromatic ring and the pyrimidine core on CRF-1 receptor binding were investigated. A number of compounds with Ki values below 10 nM and lipophilicity in a minimally acceptable range for a CNS drug (cLog P < 5) were discovered.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to Elsevier Science. |
| Keywords: | CRF-1; Anxiety; Depression; 2-Arylpyrimidine |
| ID Code: | 7135 |
| Deposited On: | 25 Oct 2010 12:30 |
| Last Modified: | 04 Feb 2011 04:57 |
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