Bioorganic & medicinal chemistry

Syntheses and evaluation of fluorinated conformationally restricted analogues of GABA as potential inhibitors of GABA aminotransferase

Z Wang, RB Silverman

Index: Wang, Zhiyong; Silverman, Richard B. Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 7 p. 2242 - 2252

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Citation Number: 24

Abstract

Inhibition of γ-aminobutyric acid aminotransferase (GABA-AT) could raise the concentration of GABA, an inhibitory neurotransmitter in the human brain, and could have therapeutic applications for a variety of neurological diseases including epilepsy. Four fluorine- containing analogues of GABA with conformations restricted by a cyclohexane ring system were designed and synthesized, but unlike some of their five-membered ring counterparts, ...