Synthesis and structure–affinity relationships of 1, 3, 5-alkylsubstituted cyclohexylamines binding at NMDA receptor PCP site

A Jirgensons, V Kauss, I Kalvinsh, MR Gold…

文献索引：Jirgensons, Aigars; Kauss, Valerjans; Kalvinsh, Ivars; Gold, Markus R.; Danysz, Wojciech; Parsons, Chris G.; Quack, Gunter European Journal of Medicinal Chemistry, 2000 , vol. 35, # 6 p. 555 - 565

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被引用次数: 15

摘要

A series of 1, 3, 5-alkylsubstituted cyclohexylamines 2 were synthesized as ligands for the N- methyl-D-aspartate (NMDA) receptor phencyclidine (PCP) binding site. Pure diastereomers with defined configuration of amino group 2-ax and 2-eq were obtained. The optimal size of 1, 3, 5-substituents was determined for cyclohexylamines 2 with an equatorial amino group in the lowest energy conformation using Hansch analysis. According to the data, the ...