Synthesis and biological evaluation of glutathione-like tripeptidesagainstTrypanosoma cruzi

Glutathionylspermidine synthase (GSS) is a crucial enzyme in the trypanothione biosynthetic pathway and is also an interesting molecular target for drug design. We synthesized a series of amides of a glutathione analogue (L-γ-Glu-L-Leu-Gly-NHR) where R are linear alkyl groups. All of these drugs exh...

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Detalles Bibliográficos
Autores principales: Ravaschino, Esteban Luis, Rodríguez, Juan Bautista
Publicado: 2003
Materias:
American trypanosomiasis
Glutathionylspermidine synthase
Trypanosoma cruzi
Trypanothione
gamma glutamyl alpha benzyl ester leucylgylcyl n 1 butylamide
gamma glutamyl alpha benzyl ester leucylgylcyl n 1 heptylamide
gamma glutamyl alpha benzyl ester leucylgylcyl n 1 hexylamide
gamma glutamyl alpha benzyl ester leucylgylcyl n 1 octylamide
gamma glutamyl alpha benzyl ester leucylgylcyl n 1 pentylamide
gamma glutamyl alpha benzyl ester leucylgylcyl n 1 propylamide
gamma glutamyl alpha benzyl ester leucylgylcyl n ethylamide
gamma glutamyl alpha benzyl ester leucylgylcyl n methylamide
glutathione derivative
glutathionylspermidine synthase
n benzyloxycarbonyl gamma glutamyl alpha benzyl ester leucylgylcyl n 1 butylamide
n benzyloxycarbonyl gamma glutamyl alpha benzyl ester leucylgylcyl n 1 heptylamide
n benzyloxycarbonyl gamma glutamyl alpha benzyl ester leucylgylcyl n 1 hexylamide
n benzyloxycarbonyl gamma glutamyl alpha benzyl ester leucylgylcyl n 1 octylamide
n benzyloxycarbonyl gamma glutamyl alpha benzyl ester leucylgylcyl n 1 pentylamide
n benzyloxycarbonyl gamma glutamyl alpha benzyl ester leucylgylcyl n 1 propylamide
n benzyloxycarbonyl gamma glutamyl alpha benzyl ester leucylgylcyl n ethylamide
n benzyloxycarbonyl gamma glutamyl alpha benzyl ester leucylgylcyl n methylamide
spermidine synthase
tripeptide derivative
unclassified drug
article
Chagas disease
drug screening
drug structure
nonhuman
peptide synthesis
Acceso en línea:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_14246376_v2003_n10_p298_Ravaschino
http://hdl.handle.net/20.500.12110/paper_14246376_v2003_n10_p298_Ravaschino
Aporte de:
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) de Universidad de Buenos Aires
Descripción
Sumario:Glutathionylspermidine synthase (GSS) is a crucial enzyme in the trypanothione biosynthetic pathway and is also an interesting molecular target for drug design. We synthesized a series of amides of a glutathione analogue (L-γ-Glu-L-Leu-Gly-NHR) where R are linear alkyl groups. All of these drugs exhibited marginal biological activity against the responsible agent of Chagas' disease, the protozoan Trypanosoma cruzi.

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