Author/Authors :
Katie Amssoms، نويسنده , , Sandra L. Oza، نويسنده , , Esteban Ravaschino، نويسنده , , Abdellah Yamani، نويسنده , , Anne-Marie Lambeir، نويسنده , , Padinchare Rajan، نويسنده , , Gunther Bal، نويسنده , , Juan Bautista Rodriguez، نويسنده , , Alan H. Fairlamb، نويسنده , , Koen Augustyns، نويسنده , , Achiel Haemers، نويسنده ,
Abstract :
Glutathionylspermidine synthetase/amidase (GspS) is an essential enzyme in the biosynthesis and turnover of trypanothione and represents an attractive target for the design of selective anti-parasitic drugs. We synthesised a series of analogues of glutathione ( γ Glu- -Leu-Gly-X) where the glycine carboxylic acid group (X) has been substituted for other acidic groups such as tetrazole, hydroxamic acid, acylsulphonamide and boronic acid. The boronic acid appears the most promising lead compound (IC50 of 17.2 μM).
