Author/Authors :
Taeyoung Yoon، نويسنده , , Stéphane De Lombaert، نويسنده , , Robbin Brodbeck، نويسنده , , Michael Gulianello، نويسنده , , James E. Krause، نويسنده , , Alan Hutchison، نويسنده , , Raymond F. Horvath، نويسنده , , Ping Ge، نويسنده , , John Kehne، نويسنده , , Diane Hoffman-Kim، نويسنده , , Jayaraman Chandrasekhar، نويسنده , , Dario Doller، نويسنده , , Kevin J. Hodgetts، نويسنده ,
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.
Keywords :
Anxiety , depression , 2-Arylpyrimidine , CRF-1
