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Wiley-VCH Verlag, ChemInform, 2(34), 2003

DOI: 10.1002/chin.200302163

Elsevier, Bioorganic and Medicinal Chemistry Letters, 18(12), p. 2553-2556

DOI: 10.1016/s0960-894x(02)00489-4

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Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase: part 1: substitution of the glycine carboxylic acid group

Journal article published in 2002 by Katie Amssoms, et A.-L. et A.-L., Sandra L. Oza, Esteban Ravaschino, Abdellah Yamani, Anne-Marie Lambeir ORCID, Padinchare Rajan, Gunther Bal, Juan Bautista Rodriguez, Juan Bautista Rodriguez ORCID, Alan H. Fairlamb, Koen Augustyns, Achiel Haemers
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This paper is available in a repository.

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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 (L-gamma-Glu-L-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 (IC(50) of 17.2 microM).