Synthesis and NK 1/NK 2 binding activities of a series of diacyl-substituted 2-arylpiperazines

DJ Blythin, X Chen, JJ Piwinski, NY Shih…

文献索引：Blythin, David J.; Chen, Xiao; Piwinski, John J.; Shih, Neng-Yang; Shue, Ho-Jane; Anthes, John C.; McPhail, Andrew T. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 21 p. 3161 - 3165

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被引用次数: 13

摘要

The synthesis and binding affinity for hNK1 and hNK2 receptors of a series of diacyl substituted 2-aryl piperazines are described. SAR evaluation led to the racemic derivative 11g as an apparent dual inhibitor. Chiral chromatographic separation of 11g led to the observation that NK1 activity was shown by one enantiomer (13a) and NK2 activity was shown by the other enantiomer (13b). X-ray crystallographic analysis of the crystalline di- ...