European journal of medicinal chemistry

Synthesis and structure–activity relationships of potential anticonvulsants based on 2-piperidinecarboxylic acid and related pharmacophores

B Ho, AM Crider, JP Stables

文献索引：Ho, Bin; Michael Crider; Stables, James P European Journal of Medicinal Chemistry, 2001 , vol. 36, # 3 p. 265 - 286

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被引用次数: 128

摘要

Using N-(2, 6-dimethyl) phenyl-2-piperidinecarboxamide (1) and N-(α-methylbenzyl)-2- piperidinecarboxamide (2) as structural leads, a variety of analogues were synthesised and evaluated for anticonvulsant activity in the MES test in mice. In the N-benzyl series, introduction of 3-Cl, 4-Cl, 3, 4-Cl2, or 3-CF3 groups on the aromatic ring led to an increase in MES activity. Replacement of the α-methyl group by either i-Pr or benzyl groups enhanced ...