AI Article Synopsis
- The study focuses on developing and analyzing a new class of CRF-1 receptor antagonists called 2-arylpyrimidines.
- Researchers examined how changes in the aromatic ring and the pyrimidine core affected the compounds' ability to bind to the CRF-1 receptor.
- Several promising compounds were found with strong binding affinity (K(i) values below 10 nM) and suitable lipophilicity for potential use in central nervous system therapies (cLogP<5).
Article 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 K(i) values below 10 nM and lipophilicity in a minimally acceptable range for a CNS drug (cLogP<5) were discovered.
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| http://dx.doi.org/10.1016/j.bmcl.2008.07.063 | DOI Listing |
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