期刊
ANTIVIRAL RESEARCH
卷 82, 期 1, 页码 89-94出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.antiviral.2009.01.003
关键词
Glycopeptide antibiotic; Ristocetin; Influenza; Antiviral
资金
- Fonds voor Wetenschappelijk Onderzoek Vlaanderen (FWO) [9.0188.07]
- International Consortium for Anti-Virals (ICAV)
- Hungarian National Scientific Research Foundation [OTKA T 46744]
Previous studies have demonstrated that glycopeptide compounds carrying hydrophobic substituents can have favorable pharmacological (i.e. antibacterial and antiviral) properties. We here report on the in vitro anti-influenza virus activity of aglycoristocetin derivatives containing hydrophobic side chain-substituted cyclobutenedione. The lead compound 8e displayed an antivirally effective concentration of 0.4 mu M, which was consistent amongst influenza A/H1N1, A/H3N2 and B viruses, and a selectivity index >= 50. Structural analogues derived from aglycovancomycin were found to be inactive. The hydrophobic side chain was shown to be an important determinant of activity. The narrow structure-activity relationship and broad activity against several human influenza viruses suggest a highly conserved interaction site, which is presumably related to the influenza virus entry process. Compound 8e proved to be inactive against several unrelated RNA and DNA viruses, except for varicella-zoster virus, against which a favorable activity was noted. (C) 2009 Elsevier B.V. All rights reserved.
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