| Literature DB >> 28068604 |
Giselle Barbosa-Lima1, Adriana M Moraes2, Adriele da S Araújo3, Emerson T da Silva3, Caroline S de Freitas4, Yasmine R Vieira1, Andressa Marttorelli4, José Cerbino Neto5, Patrícia T Bozza6, Marcus V N de Souza7, Thiago Moreno L Souza1.
Abstract
Zika virus (ZIKV), an arthropod-born Flavivirus, has been associated with a wide range of neurological diseases in adults, foetuses and neonates. Since no vaccine is available, repurposing of antiviral drugs currently in medical use is necessary. Mefloquine has confirmed anti-ZIKV activity. We used medicinal chemistry-driven approaches to synthesize and evaluate the ability of a series of new 2,8-bis(trifluoromethyl)quinoline derivatives to inhibit ZIKV replication in vitro, in order to improve the potency of mefloquine. We found that quinoline derivatives 3a and 4 were the most potent compounds within this series, both with mean EC50 values of 0.8 μM, which represents a potency 5 times that of mefloquine. These results indicate that new 2,8-bis(trifluoromethyl)quinoline chemical structures may be promising for the development of novel anti-ZIKV drugs.Entities:
Keywords: Antiviral; Mefloquine; Quinoline derivatives; Zika virus
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Year: 2016 PMID： 28068604 DOI： 10.1016/j.ejmech.2016.12.058
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514