Bioorganic & medicinal chemistry

A novel class of potent γ-aminobutyric acid aminotransferase inhibitor, 3-(hydroxyamino) propylamine and analogues

S Fushiya, T Kanazawa, S Nozoe

Index: Fushiya, Shinji; Kanazawa, Toshiyuki; Nozoe, Shigeo Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 11 p. 2089 - 2094

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Citation Number: 4

Abstract

Hydroxyamino analogues of γ-aminobutyric acid (GABA) were synthesized and evaluated for inhibitory activity toward γ-aminobutyric acid aminotransferase (GABA-T). The title compound, 3-(hydroxyamino) propylamine (HPA), showed a potent inhibitory activity. The inhibition is competitive with respect to GABA and the Ki value of GABA-T for HPA is 0.4 mmol. The activity of inhibition is comparable to those of aminoxyacetic acid and valproic ...