ArticleChembiochem : a European journal of chemical biology2015
Tobramycin Variants with Enhanced Ribosome-Targeting Activity.
Article in Chembiochem : a European journal of chemical biology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 27 citations in OpenAlex.
- Synthesis and Antibacterial Activity of New 6″-Modified Tobramycin Derivatives.Antibiotics (Basel, Switzerland) · 2024Article
- Engineering ofMolecules (Basel, Switzerland) · 2021Article
- Article
- Selective Modification of Streptozotocin at the C3 Position to Improve Its Bioactivity as Antibiotic and Reduce Its Cytotoxicity towards Insulin-Producing β Cells.Antibiotics (Basel, Switzerland) · 2020Article
- Modified Aminoglycosides Bind Nucleic Acids in High-Molecular-Weight Complexes.Antibiotics (Basel, Switzerland) · 2020Article
- Roles of specific aminoglycoside-ribosome interactions in the inhibition of translation.RNA (New York, N.Y.) · 2019Article
- Rapid Solid-phase Syntheses of Peptidic-Aminoglycoside Library.Tetrahedron · 2018Article
- Derivatives of Ribosome-Inhibiting Antibiotic Chloramphenicol Inhibit the Biosynthesis of Bacterial Cell Wall.ACS infectious diseases · 2018Article
- Differential Effects of Linkers on the Activity of Amphiphilic Tobramycin Antifungals.Molecules (Basel, Switzerland) · 2018Article
- Comprehensive review of chemical strategies for the preparation of new aminoglycosides and their biological activities.Chemical Society reviews · 2018Review
- Mechanisms of Resistance to Aminoglycoside Antibiotics: Overview and Perspectives.MedChemComm · 2016Article
- Synthesis and Bioactivities of Kanamycin B-Derived Cationic Amphiphiles.Journal of medicinal chemistry · 2015Article
- Synthesis and Biological Activity of Mono- and Di-N-acylated Aminoglycosides.ACS medicinal chemistry letters · 2015Article
- A review of patents (2011-2015) towards combating resistance to and toxicity of aminoglycosides.MedChemCommArticle
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
With the increased evolution of aminoglycoside (AG)-resistant bacterial strains, the need to develop AGs with 1) enhanced antimicrobial activity, 2) the ability to evade resistance mechanisms, and 3) the capability of targeting the ribosome with higher efficiency is more and more pressing. The chemical derivatization of the naturally occurring tobramycin (TOB) by attachment of 37 different thioether groups at the 6''-position led to the identification of generally poorer substrates of TOB-targeting AG-modifying enzymes (AMEs). Thirteen of these displayed better antibacterial activity than the parent TOB while retaining ribosome-targeting specificity. Analysis of these compounds in vitro shed light on the mechanism by which they act and revealed three with clearly enhanced ribosome-targeting activity.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.