2. Academic Validation
  3. 2,8-bis(trifluoromethyl)quinoline analogs show improved anti-Zika virus activity, compared to mefloquine

2,8-bis(trifluoromethyl)quinoline analogs show improved anti-Zika virus activity, compared to mefloquine

  • Eur J Med Chem. 2017 Feb 15:127:334-340. doi: 10.1016/j.ejmech.2016.12.058.
Giselle Barbosa-Lima 1,  Adriana M Moraes 2,  Adriele da S Araújo 3,  Emerson T da Silva 3,  Caroline S de Freitas 4,  Yasmine R Vieira 1,  Andressa Marttorelli 4,  José Cerbino Neto 5,  Patrícia T Bozza 6,  Marcus V N de Souza 7,  Thiago Moreno L Souza 1
Affiliations

Affiliations

  • 1 Instituto Oswaldo Cruz, Fiocruz - Fundação Oswaldo Cruz, Rio de Janeiro, Brazil; Centro de Desenvolvimento Tecnológico em Saúde, Fiocruz - Fundação Oswaldo Cruz, Rio de Janeiro, Brazil; Instituto Nacional de Infectologia Evandro Chagas, Fiocruz - Fundação Oswaldo Cruz, Rio de Janeiro, Brazil.
  • 2 Instituto de Tecnologia em Fármacos - Far-Manguinhos, Fiocruz - Fundação Oswaldo Cruz, Rio de Janeiro, Brazil; Departamento de Química Orgânica, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil.
  • 3 Instituto de Tecnologia em Fármacos - Far-Manguinhos, Fiocruz - Fundação Oswaldo Cruz, Rio de Janeiro, Brazil.
  • 4 Instituto Oswaldo Cruz, Fiocruz - Fundação Oswaldo Cruz, Rio de Janeiro, Brazil; Centro de Desenvolvimento Tecnológico em Saúde, Fiocruz - Fundação Oswaldo Cruz, Rio de Janeiro, Brazil.
  • 5 Instituto Nacional de Infectologia Evandro Chagas, Fiocruz - Fundação Oswaldo Cruz, Rio de Janeiro, Brazil.
  • 6 Instituto Oswaldo Cruz, Fiocruz - Fundação Oswaldo Cruz, Rio de Janeiro, Brazil.
  • 7 Instituto de Tecnologia em Fármacos - Far-Manguinhos, Fiocruz - Fundação Oswaldo Cruz, Rio de Janeiro, Brazil; Departamento de Química Orgânica, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil. Electronic address: marcos_souza@far.fiocruz.br.
PMID: 28068604 DOI: 10.1016/j.ejmech.2016.12.058
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.

Keywords

Antiviral; Mefloquine; Quinoline derivatives; Zika virus.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z