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Eur J Med Chem ; 127: 334-340, 2017 Feb 15.
Article in English | MEDLINE | ID: mdl-28068604

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.


Subject(s)
Antiviral Agents/chemistry , Antiviral Agents/pharmacology , Mefloquine/pharmacology , Quinolines/chemistry , Quinolines/pharmacology , Zika Virus/drug effects , Animals , Antiviral Agents/chemical synthesis , Antiviral Agents/toxicity , Chlorocebus aethiops , Drug Design , Quinolines/chemical synthesis , Quinolines/toxicity , Structure-Activity Relationship , Vero Cells , Virus Replication/drug effects , Zika Virus/physiology
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