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Vancomycin-Lipopeptide Conjugates with High Antimicrobial Activity on Vancomycin-Resistant Enterococci
Open AccessArticle

Reprogramming of the Antibacterial Drug Vancomycin Results in Potent Antiviral Agents Devoid of Antibacterial Activity

1
Department of Pharmaceutical Chemistry, University of Debrecen, Egyetem tér 1, H-4032 Debrecen, Hungary
2
Doctoral School of Pharmaceutical Sciences, University of Debrecen, Egyetem tér 1, H-4032 Debrecen, Hungary
3
Rega Institute for Medical Research, KU Leuven, B-3000 Leuven, Belgium
4
Department of Medical Microbiology, Semmelweis University, Nagyvárad tér 4, H-1089 Budapest, Hungary
5
Department of Organic Chemistry, University of Debrecen, H-4032 Debrecen, Hungary
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2020, 13(7), 139; https://doi.org/10.3390/ph13070139
Received: 21 May 2020 / Revised: 25 June 2020 / Accepted: 26 June 2020 / Published: 29 June 2020
(This article belongs to the Special Issue Glycopeptide Antibiotics 2020)
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. View Full-Text
Keywords: glycopeptide antibiotic; vancomycin aglycone hexapeptide; antiviral; influenza virus; human coronavirus glycopeptide antibiotic; vancomycin aglycone hexapeptide; antiviral; influenza virus; human coronavirus
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MDPI and ACS Style

Szűcs, Z.; Naesens, L.; Stevaert, A.; Ostorházi, E.; Batta, G.; Herczegh, P.; Borbás, A. Reprogramming of the Antibacterial Drug Vancomycin Results in Potent Antiviral Agents Devoid of Antibacterial Activity. Pharmaceuticals 2020, 13, 139.

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