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ID: ALA1156589
Journal: Bioorg Med Chem Lett
Title: 2-Arylpyrimidines: novel CRF-1 receptor antagonists.
Authors: Yoon T, De Lombaert S, Brodbeck R, Gulianello M, Krause JE, Hutchison A, Horvath RF, Ge P, Kehne J, Hoffman D, Chandrasekhar J, Doller D, Hodgetts KJ.
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.
CiteXplore: 18672365