620179-01-3Relevant articles and documents
Synthesis and SAR of 8-arylquinolines as potent corticotropin-releasing factor1 (CRF1) receptor antagonists
Huang, Charles Q.,Wilcoxen, Keith,McCarthy, James R.,Haddach, Mustapha,Webb, Thomas R.,Gu, Jian,Xie, Yun-Feng,Grigoriadis, Dimitri E.,Chen, Chen
, p. 3375 - 3379 (2007/10/03)
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.