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Antiviral evaluation of 1,4-disubstituted-1,2,3-triazole derivatives against Chikungunya virus.
Rabelo, Vitor Won-Held; da Silva, Verônica Diniz; Sanchez Nuñez, Maria Leonisa; Dos Santos Corrêa Amorim, Leonardo; Buarque, Camilla Djenne; Kuhn, Richard J; Abreu, Paula Alvarez; Nunes de Palmer Paixão, Izabel Christina.
  • Rabelo VW; Programa de Pós-graduação em Ciências e Biotecnologia, Instituto de Biologia, Universidade Federal Fluminense, Niterói, RJ, CEP, 24210-201, Brazil.
  • da Silva VD; Laboratório de Síntese Orgânica, Pontifícia Universidade Católica do Rio de Janeiro, Rio de Janeiro, RJ, CEP, 22451-900, Brazil.
  • Sanchez Nuñez ML; Programa de Pós-graduação em Ciências e Biotecnologia, Instituto de Biologia, Universidade Federal Fluminense, Niterói, RJ, CEP, 24210-201, Brazil.
  • Dos Santos Corrêa Amorim L; Programa de Pós-graduação em Ciências e Biotecnologia, Instituto de Biologia, Universidade Federal Fluminense, Niterói, RJ, CEP, 24210-201, Brazil.
  • Buarque CD; Gerência de Desenvolvimento Tecnológico, Instituto Vital Brazil, Niterói, RJ, 24230-410, Brazil.
  • Kuhn RJ; Laboratório de Síntese Orgânica, Pontifícia Universidade Católica do Rio de Janeiro, Rio de Janeiro, RJ, CEP, 22451-900, Brazil.
  • Abreu PA; Department of Biological Sciences, Purdue University, West Lafayette, IN 47907, USA.
  • Nunes de Palmer Paixão IC; Purdue Institute of Inflammation, Immunology, & Infectious Disease, Purdue University, West Lafayette, IN 47907, USA.
Future Virol ; 18(13): 865-880, 2023 Sep.
Article en En | MEDLINE | ID: mdl-37974899
ABSTRACT

Aim:

This work aimed to investigate the antiviral activity of two 1,4-disubstituted-1,2,3-triazole derivatives (1 and 2) against Chikungunya virus (CHIKV) replication. Materials &

methods:

Cytotoxicity was analyzed using colorimetric assays and the antiviral potential was evaluated using plaque assays and computational tools.

Results:

Compound 2 showed antiviral activity against CHIKV 181-25 in BHK-21 and Vero cells. Also, this compound presented a higher activity against CHIKV BRA/RJ/18 in Vero cells, like compound 1. Compound 2 exhibited virucidal activity and inhibited virus entry while compound 1 inhibited virus release. Molecular docking suggested that these derivatives inhibit nsP1 protein while compound 1 may also target capsid protein.

Conclusion:

Both compounds exhibit promising antiviral activity against CHIKV by blocking different steps of virus replication.
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