| Literature DB >> 12951129 |
Charles Q Huang1, Keith Wilcoxen, James R McCarthy, Mustapha Haddach, Thomas R Webb, Jian Gu, Yun-Feng Xie, Dimitri E Grigoriadis, Chen Chen.
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.Entities:
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Year: 2003 PMID： 12951129 DOI： 10.1016/s0960-894x(03)00684-x
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823