Synthesis of Antiviral Perfluoroalkyl Derivatives of Teicoplanin and Vancomycin.


Journal

ChemMedChem
ISSN: 1860-7187
Titre abrégé: ChemMedChem
Pays: Germany
ID NLM: 101259013

Informations de publication

Date de publication:
03 09 2020
Historique:
received: 22 04 2020
revised: 28 06 2020
pubmed: 12 7 2020
medline: 17 12 2020
entrez: 12 7 2020
Statut: ppublish

Résumé

The limited scope of antiviral drugs and increasing problem of antiviral drug resistance represent a global health threat. Glycopeptide antibiotics and their lipophilic derivatives have emerged as relevant inhibitors of diverse viruses. Herein, we describe a new strategy for the synthesis of dual hydrophobic and lipophobic derivatives of glycopeptides to produce selective antiviral agents without membrane-disrupting activity. Perfluorobutyl and perfluorooctyl moieties were attached through linkers of different length to azido derivatives of vancomycin aglycone and teicoplanin pseudoaglycone, and the new derivatives were evaluated against a diverse panel of viruses. The teicoplanin derivatives displayed strong anti-influenza virus activity at nontoxic concentrations. Some of the perfluoroalkylated glycopeptides were also active against a few other viruses such as herpes simplex virus or coronavirus. These data encourage further exploration of glycopeptide analogues for broad antiviral application.

Identifiants

pubmed: 32652783
doi: 10.1002/cmdc.202000260
pmc: PMC7540527
doi:

Substances chimiques

Anti-Bacterial Agents 0
Antiviral Agents 0
Fluorocarbons 0
Palladium 5TWQ1V240M
Teicoplanin 61036-62-2
Vancomycin 6Q205EH1VU

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

1661-1671

Subventions

Organisme : European Regional Development Fund
ID : GINOP-2.3.2-15-2016-00044
Pays : International
Organisme : European Regional Development Fund
ID : GINOP-2.3.2-15-2016-00008
Pays : International
Organisme : European Regional Development Fund
ID : GINOP-2.3.3-15-2016-00004
Pays : International
Organisme : European Social Fund
ID : EFOP-3.6.3-VEKOP-16-2017-00009
Pays : International
Organisme : National Research, Development and Innovation Office of Hungary
ID : K119509
Pays : International

Informations de copyright

© 2020 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA.

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Auteurs

Ilona Bereczki (I)

Department of Pharmaceutical Chemistry, University of Debrecen, Egyetem tér 1, 4032, Debrecen, Hungary.

Magdolna Csávás (M)

Department of Pharmaceutical Chemistry, University of Debrecen, Egyetem tér 1, 4032, Debrecen, Hungary.

Zsolt Szűcs (Z)

Department of Pharmaceutical Chemistry, University of Debrecen, Egyetem tér 1, 4032, Debrecen, Hungary.
Doctoral School of Pharmaceutical Sciences, University of Debrecen, Egyetem tér 1, 4032, Debrecen, Hungary.

Erzsébet Rőth (E)

Department of Pharmaceutical Chemistry, University of Debrecen, Egyetem tér 1, 4032, Debrecen, Hungary.

Gyula Batta (G)

Department of Organic Chemistry, University of Debrecen, Egyetem tér 1, 4032, Debrecen, Hungary.

Eszter Ostorházi (E)

Department of Medical Microbiology, Semmelweis University, Mária u. 41, 1085, Budapest, Hungary.

Lieve Naesens (L)

Rega Institute for Medical Research, KU Leuven, 3000, Leuven, Belgium.

Anikó Borbás (A)

Department of Pharmaceutical Chemistry, University of Debrecen, Egyetem tér 1, 4032, Debrecen, Hungary.

Pál Herczegh (P)

Department of Pharmaceutical Chemistry, University of Debrecen, Egyetem tér 1, 4032, Debrecen, Hungary.

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Classifications MeSH