Development of novel regulators for controlling glutathione biosynthesis

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This research is aimed to develop novel antiinfective drugs using (2S)-2-amino-4-(2-carboxybutylsulfonimidoyl) butyric acid, a potent γ-glutamylcysteine synthetase (γ-GCS) inhibitor, as a precursor. Hydrophobic amino acids were conjugated to N-terminal of the lead compound. The synthetic prodrugs significantly decreased glutathione content of E. coli as compared to the precursor. This result suggested that 1) these prodrugs were uptaken into E.coli and decomposed by peptidases, and 2) the liberated inhibitor inactivated E.coli γ-GCS in situ.