European journal of medicinal chemistry · 2016
2,8-bis(trifluoromethyl)quinoline analogs show improved anti-Zika virus activity, compared to mefloquine.
Сравнительное исследованиеСтатьяНазвание и аннотация: Перевод в очереди
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Barbosa-Lima Giselle, Moraes Adriana M, Araújo Adriele da S, da Silva Emerson T, de Freitas Caroline S, Vieira Yasmine R, Marttorelli Andressa, Neto José Cerbino, Bozza Patrícia T, de Souza Marcus V N, Souza Thiago Moreno L
Аннотация
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.