Synthesis and SAR of 8-arylquinolines as potent corticotropin-releasing factor1 (CRF1) receptor antagonists |
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| Authors: | Huang Charles Q Wilcoxen Keith McCarthy James R Haddach Mustapha Webb Thomas R Gu Jian Xie Yun-Feng Grigoriadis Dimitri E Chen Chen |
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| Affiliation: | Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 10555 Science Centre Drive, San Diego, CA 92121, USA. |
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| 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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