Inhibition and substrate activity of conformationally rigid vigabatrin analogues with γ-aminobutyric acid aminotransferase

…, JM Pingsterhaus, RB Silverman

文献索引：Qiu, Jian; Pingsterhaus, Joyce M.; Silverman, Richard B. Journal of Medicinal Chemistry, 1999 , vol. 42, # 22 p. 4725 - 4728

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被引用次数: 35

摘要

Several cyclopentene GABA analogues were synthesized as conformationally rigid analogues of the epilepsy drug vigabatrin and tested as inhibitors and substrates of γ- aminobutyric acid aminotransferase (GABA-AT). None of these compounds produced time- dependent inhibition.(1 R, 4 S)-(+)-4-Amino-2-cyclopentene-1-carboxylic acid ((+)-3),(4 R)-(- )-4-amino-1-cyclopentene-1-carboxylic acid ((-)-4), and d, l-3-amino-1-cyclopentene-1- ...