215115-07-4Relevant academic research and scientific papers
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 (2003)
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.
CRF antagonistic quino- and quinazolines
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, (2008/06/13)
This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1is C1-6alkyl, NR6R7, OR6or SR7; Rsu
