Author/Authors :
Charles Q. Huang، نويسنده , , Keith Wilcoxen، نويسنده , , James R. McCarthy، نويسنده , , Mustapha Haddach، نويسنده , , Thomas R. Webb، نويسنده , , Jian Gu، نويسنده , , Yun-Feng Xie، نويسنده , , Dimitri E. Grigoriadis، نويسنده , , Chen Chen، نويسنده ,
Abstract :
A series of 4-substituted 8-aryl-2-methylquinolines 4 was designed and synthesized as highly potent antagonists for the human CRF1 receptor. This series of compounds displayed parallel SAR to other bicyclic systems such as pyrazolo[1,5-a]pyrimidines, with several compounds possessing low nanomolar binding affinity. In addition to the high potency, the basicity of this 4-aminoquinoline core may offer CRF1 antagonists with lower lipophilicity.
