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Título

A Simple Structural-Based Approach to Prevent Aminoglycoside Inactivation by Bacterial Defense Proteins. Conformational Restriction Provides Effective Protection against Neomycin-B Nucleotidylation by ANT4

AutorAsensio, Juan Luis ; Hidalgo, Ana; Bastida, Agatha; Torrado, Mario; Corzana, Francisco; Chiara, José Luis ; García-Junceda, Eduardo ; Cañada, F. Javier ; Jiménez-Barbero, Jesús
Fecha de publicación2005
EditorAmerican Chemical Society
CitaciónJournal of the American Chemical Society 127(23): 8278-8279 (2005)
ResumenHerein, we describe how the conformational differences exhibited by aminoglycosides in the binding pockets of the ribosome and those enzymes involved in bacterial resistance can be exploited in the design of new antibiotic derivatives with improved activity in resistant strains. The simple modification shown in the figure, leading to the conformationally restricted 5, provides an effective protection against aminoglycoside inactivation by Staphylococcus aureus ANT4, both in vivo and in vitro.
Descripción2 páginas, 3 figuras, 1 esquema.-- Supporting Information Available: Extended experimental details about the design, synthesis, NMR and computational analysis, and enzymatic and biological testing of 5. This material is available free of charge via the Internet at http://pubs.acs.org.
Versión del editorhttp://dx.doi.org/10.1021/ja051722z
URIhttp://hdl.handle.net/10261/30951
DOI10.1021/ja051722z
ISSN0002-7863
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