Special Issue "Glycopeptide Antibiotics 2020"

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 31 October 2020.

Special Issue Editor

Dr. Magdolna Csávás
Website SciProfiles
Guest Editor
Department of Pharmaceutical Chemistry, University of Debrecen, Debrecen, Hungary
Interests: glycopeptides; antibiotics; synthesis; antibacterial activity; mechanism of action; antibiotic resistance

Special Issue Information

Dear Colleagues,

As Guest Editor, I kindly invite you to submit a manuscript to the Special Issue “Glycopeptide Antibiotics”, which will be published in Pharmaceuticals. The Special Issue focuses on all topics related to glycopeptide antibiotics: the (semi)synthetic modification of glycopeptides; investigation of the mechanism of action; antibiotic resistance related topics; studies on antibacterial or antimicrobial activity of glycopeptides; structure determination and spectroscopic issues.

You may submit your manuscript until 31 October 2020. Authors are also encouraged to send a tentative title or/and short abstract for a record.

We sincerely hope that you or a member of your laboratory will be able to contribute.

Dr. Magdolna Csávás
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

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. Pharmaceuticals 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 1400 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.

Keywords

  • glycopeptides
  • antibiotics
  • synthesis
  • antibacterial activity
  • mechanism of action
  • antibiotic resistance

Published Papers (2 papers)

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Research

Open AccessArticle
Reprogramming of the Antibacterial Drug Vancomycin Results in Potent Antiviral Agents Devoid of Antibacterial Activity
Pharmaceuticals 2020, 13(7), 139; https://doi.org/10.3390/ph13070139 - 29 Jun 2020
Abstract
Influenza A and B viruses are a global threat to human health and increasing resistance to the existing antiviral drugs necessitates new concepts to expand the therapeutic options. Glycopeptide derivatives have emerged as a promising new class of antiviral agents. To avoid potential [...] Read more.
Influenza A and B viruses are a global threat to human health and increasing resistance to the existing antiviral drugs necessitates new concepts to expand the therapeutic options. Glycopeptide derivatives have emerged as a promising new class of antiviral agents. To avoid potential antibiotic resistance, these antiviral glycopeptides are preferably devoid of antibiotic activity. We prepared six vancomycin aglycone hexapeptide derivatives with the aim of obtaining compounds having anti-influenza virus but no antibacterial activity. Two of them exerted strong and selective inhibition of influenza A and B virus replication, while antibacterial activity was successfully eliminated by removing the critical N-terminal moiety. In addition, these two molecules offered protection against several other viruses, such as herpes simplex virus, yellow fever virus, Zika virus, and human coronavirus, classifying these glycopeptides as broad antiviral molecules with a favorable therapeutic index. Full article
(This article belongs to the Special Issue Glycopeptide Antibiotics 2020)
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Open AccessArticle
Vancomycin-Lipopeptide Conjugates with High Antimicrobial Activity on Vancomycin-Resistant Enterococci
Pharmaceuticals 2020, 13(6), 110; https://doi.org/10.3390/ph13060110 - 29 May 2020
Abstract
Multidrug-resistant bacteria represent one of the most important health care problems worldwide. While there are numerous drugs available for standard therapy, there are only a few compounds capable of serving as a last resort for severe infections. Therefore, approaches to control multidrug-resistant bacteria [...] Read more.
Multidrug-resistant bacteria represent one of the most important health care problems worldwide. While there are numerous drugs available for standard therapy, there are only a few compounds capable of serving as a last resort for severe infections. Therefore, approaches to control multidrug-resistant bacteria must be implemented. Here, a strategy of reactivating the established glycopeptide antibiotic vancomycin by structural modification with polycationic peptides and subsequent fatty acid conjugation to overcome the resistance of multidrug-resistant bacteria was followed. This study especially focuses on the structure–activity relationship, depending on the modification site and fatty acid chain length. The synthesized conjugates showed high antimicrobial potential on vancomycin-resistant enterococci. We were able to demonstrate that the antimicrobial activity of the vancomycin-lipopeptide conjugates depends on the chain length of the attached fatty acid. All conjugates showed good cytocompatibility in vitro and in vivo. Radiolabeling enabled the in vivo determination of pharmacokinetics in Wistar rats by molecular imaging and biodistribution studies. An improved biodistribution profile in comparison to unmodified vancomycin was observed. While vancomycin is rapidly excreted by the kidneys, the most potent conjugate shows a hepatobiliary excretion profile. In conclusion, these results demonstrate the potential of the structural modification of already established antibiotics to provide highly active compounds for tackling multidrug-resistant bacteria. Full article
(This article belongs to the Special Issue Glycopeptide Antibiotics 2020)
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