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. 2003 Oct 6;13(19):3375-9.
doi: 10.1016/s0960-894x(03)00684-x.

Synthesis and SAR of 8-arylquinolines as potent corticotropin-releasing factor1 (CRF1) receptor antagonists

Charles Q Huang  1 , Keith Wilcoxen, James R McCarthy, Mustapha Haddach, Thomas R Webb, Jian Gu, Yun-Feng Xie, Dimitri E Grigoriadis, Chen Chen
Affiliations

Synthesis and SAR of 8-arylquinolines as potent corticotropin-releasing factor1 (CRF1) receptor antagonists

Charles Q Huang et al. Bioorg Med Chem Lett. .

Abstract

A series of 4-substituted 8-aryl-2-methylquinolines 4 was designed and synthesized as highly potent antagonists for the human CRF(1) 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 CRF(1) antagonists with lower lipophilicity.

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