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New and versatile approaches to the synthesis of CPP-related competitive NMDA antagonists. Preliminary structure activity relationships and pharmacological …

…, G Johnson, LJ Brahce, LL Coughenour

文献索引:Hays; Bigge; Novak; Drummond; Bobovski; Rice; Johnson; Brahce; Coughenour Journal of Medicinal Chemistry, 1990 , vol. 33, # 10 p. 2916 - 2924

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被引用次数: 39

摘要

Fourteen new CPP analogues have been prepared with methyl 1-(phenylmethyl)(= k)-1, 2- piperazinedicarboxylate 3 as a versatile synthetic intermediate. Derivatives were evaluated as NMDA ligands by their ability to displace [3H] CPP from rat cortical membranes. The binding affinity of various chain lengths at the N4-position of the CPP analogues, 5a, 5b, and 9a mimica the binding affinity observed for the acyclic derivatives AP6, AP8, and AP5. ...