2,8-bis(trifluoromethyl)quinoline analogs show improved anti-Zika virus activity, compared to mefloquine
| Autor: | Thiago Moreno L. Souza, Caroline S. de Freitas, Emerson Teixeira da Silva, José Cerbino Neto, Giselle Barbosa-Lima, Patrícia T. Bozza, Andressa Marttorelli, Adriana Marques Moraes, Marcus V. N. de Souza, Adriele da Silva Araújo, Yasmine Rangel Vieira |
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| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Pharmacology Virus Replication Antiviral Agents Zika virus Structure-Activity Relationship 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Chlorocebus aethiops Drug Discovery medicine Animals Potency 030212 general & internal medicine Vero Cells EC50 Trifluoromethyl biology Chemistry Mefloquine Organic Chemistry Quinoline Zika Virus General Medicine biology.organism_classification Virology Flavivirus 030104 developmental biology Drug Design Quinolines medicine.drug |
| Zdroj: | European Journal of Medicinal Chemistry. 127:334-340 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2016.12.058 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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