Thio Modified Aminoglycoside Antibiotic Analogs

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

Manuscript Submission Information

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Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Antibiotics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

• thio-neamine
• aminoglycosides
• thio-functionalization
• antimicrobial resistance
• phosphorylases
• adenylases
• acetylases
• gramm-negative bacteria
• kanamycin B