1624627-58-2Relevant academic research and scientific papers
MODIFIED AMINOGLYCOSIDE COMPOUNDS AND USES THEREOF IN DISABLING BACTERIAL RIBOSOME
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, (2020/06/10)
Modified aminoglycoside compounds represented by Formula I as defined and described in the specification are provided. The modified aminoglycosides feature a diamine-containing functional moiety at one or more of positions 3', 4' and 6'. Uses of the modified aminoglycosides as antimicrobial (e.g., antibacterial) agents, and in treating medical conditions associated with microorganisms, are also provided.
Towards Catalytic Antibiotics: Redesign of Aminoglycosides To Catalytically Disable Bacterial Ribosomes
Smolkin, Boris,Khononov, Alina,Pieńko, Tomasz,Shavit, Michal,Belakhov, Valery,Trylska, Joanna,Baasov, Timor
, p. 247 - 259 (2019/01/04)
The emergence of multidrug-resistant pathogens that are resistant to the majority of currently available antibiotics is a significant clinical problem. The development of new antibacterial agents and novel approaches is therefore extremely important. We set out to explore the potential of catalytic antibiotics as a new paradigm in antibiotics research. Herein, we describe our pilot study on the design, synthesis, and biological testing of a series of new derivatives of the natural aminoglycoside antibiotic neomycin B for their potential action as catalytic antibiotics. The new derivatives showed significant antibacterial activity against wild-type bacteria and were especially potent against resistant and pathogenic strains including Pseudomonas aeruginosa and methicillin-resistant Staphylococcus aureus. Selected compounds displayed RNase activity even though the activity was not as high and specific as we would have expected. On the basis of the observed chemical and biochemical data, along with the comparative molecular dynamics simulations of the prokaryotic rRNA decoding site, we postulate that the rational design of catalytic antibiotics should involve not only their structure but also a comprehensive analysis of the rRNA A-site dynamics.
Synthesis of 4′-deoxy-4′-fluoro neamine and 4′-deoxy-4′-fluoro 4′-epi neamine
Hanessian, Stephen,Saavedra, Oscar M.,Vilchis-Reyes, Miguel A.,Llaguno-Rueda, Ana M.
, p. 1166 - 1171 (2014/08/05)
The syntheses of 4′-deoxy-4′-fluoro neamine and 4′-deoxy-4′-fluoro 4′-epi neamine from the readily available neamine and paromamine are described. Different approaches for the introduction of fluorine such as the use of DAST, sulfonic esters displacement,
