Simplistic perylene-related compounds as inhibitors of tick-borne encephalitis virus reproduction.
Bioorg Med Chem Lett
; 30(10): 127100, 2020 05 15.
Article
em En
| MEDLINE
| ID: mdl-32199731
ABSTRACT
Rigid amphipathic fusion inhibitors are potent broad-spectrum antivirals based on the perylene scaffold, usually decorated with a hydrophilic group linked via ethynyl or triazole. We have sequentially simplified these structures by removing sugar moiety, then converting uridine to aniline, then moving to perylenylthiophenecarboxylic acids and to perylenylcarboxylic acid. All these polyaromatic compounds, as well as antibiotic heliomycin, still showed pronounced activity against tick-borne encephalitis virus (TBEV) with limited toxicity in porcine embryo kidney (PEK) cell line. 5-(Perylen-3-yl)-2-thiophenecarboxylic acid (5a) showed the highest antiviral activity with 50% effective concentration of approx. 1.6 nM.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Antivirais
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Perileno
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Carrapatos
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Vírus da Encefalite Transmitidos por Carrapatos
Limite:
Animals
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article