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

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• 作者：Juan Luis Asensio ; Ana Hidalgo ; Agatha Bastida ; Mario Torrado ; Francisco Corzana ; Jose Luis Chiara ; Eduardo Garc&iacute ; a-Junceda ; Javier Cañ ; ada ; and Jesú ; s Jimé ; nez-Barbero
• 刊名：Journal of the American Chemical Society
• 出版年：2005
• 出版时间：June 15, 2005
• 年：2005
• 卷：127
• 期：23
• 页码：8278 - 8279
• 全文大小：96K
• 年卷期：v.127,no.23(June 15, 2005)
• ISSN：1520-5126

文摘

Herein, 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.