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Synthesis and biological evaluation of 4-fluoroproline and 4-fluoropyrrolidine-2-acetic acid derivatives as new GABA uptake inhibitors

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Synthesis and biological evaluation of 4-fluoroproline and 4-fluoropyrrolidine-2-acetic acid derivatives as new GABA uptake inhibitors

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作者
Weiping Zhuang;Xueqing Zhao;Gang Zhao;Lihe Guo;Yunyang Lian;Jingming Zhou;Dongsheng Fang*
刊物名称
Bioorganic & Medicinal Chemistry
2009
17
18
6540-6546

{Author}: Weiping Zhuang;Xueqing Zhao;Gang Zhao;Lihe Guo;Yunyang Lian;Jingming Zhou;Dongsheng Fang*

{Journal}: Bioorganic & Medicinal Chemistry

{Year}: 2009

{Volume}: 17

{Issue}: 18

{Pages}: 6540-6546

{Keywords}:GABA uptake inhibitor;GAT-1;4-Fluoropyroline;4-Fluoropyrrolidine-2-acetic acid

{Abstract}: Preparation for the N-alkylated derivatives of enantiomerically pure (2 S )-4-fluoroproline and (2 S )-4-fluoropyrrolidine-2-acetic acid is described. The final compounds were evaluated as potential GAT-1 uptake inhibitors via cultured cell lines expressing mouse GAT-1. Compared with their corresponding 4-hydroxy compounds, these derivatives exhibited slight improvement on their inhibitory potency, but still much weaker than their corresponding compounds with no substituents at the C-4 of the pyrrolidine moiety, with the most potent affinity being about 1/15 fold as that of Tiagabine. The drastic decrease of their affinity may arise from sharp reduction of their basicity due to strong inductive effect of the 4-fluorine. However the configuration of the C-4 linking fluorine did not have much influence on their affinity for GAT-1.

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