Zheng Jianbin, Wen Ren, Luo Xiaomin, Lin Guoqiang, Zhang Jiange, Xu Linfeng, Guo Lihe, Jiang Hualiang
Department of Medicinal Chemistry, Fudan University, Shanghai 200032, China.
Bioorg Med Chem Lett. 2006 Jan 1;16(1):225-7. doi: 10.1016/j.bmcl.2005.09.004. Epub 2005 Oct 21.
Twenty novel N-diarylalkenyl-piperidinecarboxylic acid derivatives were synthesized and evaluated as gamma-aminobutyric acid uptake inhibitors. The biological assay showed that (R)-1-[4,4-bis(3-phenoxymethyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic hydrochloride possessed almost as strong GAT1 inhibitory activity as tiagabine. The synthesis and structure-activity relationships are discussed.
合成了20种新型N-二芳基烯基-哌啶羧酸衍生物，并将其作为γ-氨基丁酸摄取抑制剂进行了评估。生物学试验表明，（R）-1-[4,4-双（3-苯氧甲基-2-噻吩基）-3-丁烯基]-3-哌啶羧酸盐酸盐具有与噻加宾几乎一样强的GAT1抑制活性。本文讨论了其合成方法及构效关系。
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