Synthesis and preliminary biochemical evaluation of novel derivatives of PCP

…, DC Furlano, MV Mattson, AE Jacobson…

文献索引：Linders, Joannes T. M.; Furlano, David C.; Mattson, Mariena V.; Jacobson, Arthur E.; Rice, Kenner C. Letters in Drug Design and Discovery, 2010 , vol. 7, # 2 p. 79 - 87

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被引用次数: 4

摘要

(±)-Trans-Ph/Et and (±)-cis-Ph/Et 1-(2-ethyl-1-phenylcyclohexyl) piperidine were synthesized from 2-ethylcyclohexanone. In contrast to the corresponding trans-substituted 2- methyl compound which is 5x more potent than PCP, the trans-2-ethyl derivative has a 75x lower affinity for the PCP binding site. The cis-2-ethyl isomer is inactive like the cis-2-methyl derivative.(±)-1-(1-Phenylcyclohexyl)-2-methylpiperidine is almost as active as the parent ...