Thio Modified Aminoglycoside Antibiotic Analogs
A special issue of Antibiotics (ISSN 2079-6382).
Deadline for manuscript submissions: closed (30 November 2021) | Viewed by 458
Special Issue Editor
Special Issue Information
Dear Colleagues,
Aminoglycoside antibiotics represent a clinically important class of antibiotics, with broad activity against many strains of Gram-negative bacteria. However, pathogens with the resistant strains code for enzymes will often inactivate various aminoglycoside antibiotics via enzymatic phosphorylation, acetylation or adenylation.
The early studies of aminocyclitol antibiotics by K.L. Reinehart and T. Suami provided some insight for overcoming the bacterial resistance and gave hints helping to design products with a better antibacterial activity. One of the relevant structure modifications is thio-functionalization.
Indeed, insertion of a sulfur bridge at the specifically designated sugar unit will potentially create molecules that are more biologically active, stable, and hopefully less inactivated by specific enzymes. For example, the introduction of a thio-ether functionality at a strategic position of the core structure of neamine, a component of neomycin and kanamycin B, renders resistance to inactivation by preventing enzymatic phosphorylation, acetylation or adenylation.
The main subject of this Special Issue includes articles on specific modification of core structure of the antibiotic unit through thio-functionalization or other functional group modifications. This Special Issue seeks manuscript submissions that further our understanding of antimicrobial resistance by building prototype molecules with little or no resistance at all.
In addition, manuscripts describing other structure-related areas of core unit modifications of aminoglycosides are also very welcome.
Dr. Zbigniew J. Witczak
Guest Editor
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Keywords
- thio-neamine
- aminoglycosides
- thio-functionalization
- antimicrobial resistance
- phosphorylases
- adenylases
- acetylases
- gramm-negative bacteria
- kanamycin B
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