Artículo
Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 1: Substitution of the glycine carboxylic acid group
Amssoms, Katie; Oza, Sandra L.; Ravaschino, Esteban; Yamani, Abdellah; Lambeir, Anne Marie; Rajan, Padinchare; Bal, Gunther; Rodriguez, Juan Bautista
; Fairlamb, Alan H.; Augustyns, Koen; Haemers, Achiel
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Fecha de publicación:
09/2002
Editorial:
Pergamon-Elsevier Science Ltd
Revista:
Biorganic and Medicinal Chemistry Letters
ISSN:
0960-894X
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
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-γ-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 (IC50 of 17.2 μM).
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Articulos(UMYMFOR)
Articulos de UNID.MICROANAL.Y MET.FISICOS EN QUIM.ORG.(I)
Articulos de UNID.MICROANAL.Y MET.FISICOS EN QUIM.ORG.(I)
Citación
Amssoms, Katie; Oza, Sandra L.; Ravaschino, Esteban; Yamani, Abdellah; Lambeir, Anne Marie; et al.; Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 1: Substitution of the glycine carboxylic acid group; Pergamon-Elsevier Science Ltd; Biorganic and Medicinal Chemistry Letters; 12; 18; 9-2002; 2553-2556
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