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
Programa de Pós-graduação em Ciências e Biotecnologia, Instituto de Biologia, Universidade Federal Fluminense, Niterói, RJ, CEP, 24210-201, Brazil.
Laboratório de Síntese Orgânica, Pontifícia Universidade Católica do Rio de Janeiro, Rio de Janeiro, RJ, CEP, 22451-900, Brazil.
Future Virol. 2023 Sep;18(13):865-880. doi: 10.2217/fvl-2023-0142. Epub 2023 Oct 25.
This work aimed to investigate the antiviral activity of two 1,4-disubstituted-1,2,3-triazole derivatives ( and ) 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.
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.
Both compounds exhibit promising antiviral activity against CHIKV by blocking different steps of virus replication.
本研究旨在探究两种1,4 - 二取代 - 1,2,3 - 三唑衍生物（和）对基孔肯雅病毒（CHIKV）复制的抗病毒活性。
使用比色法分析细胞毒性，并使用蚀斑试验和计算工具评估抗病毒潜力。
化合物2在BHK - 21和Vero细胞中对CHIKV 181 - 25显示出抗病毒活性。此外，与化合物1一样，该化合物在Vero细胞中对CHIKV BRA/RJ/18表现出更高的活性。化合物2表现出杀病毒活性并抑制病毒进入，而化合物1抑制病毒释放。分子对接表明这些衍生物抑制nsP1蛋白，而化合物1也可能靶向衣壳蛋白。
两种化合物均通过阻断病毒复制的不同步骤，对CHIKV表现出有前景的抗病毒活性。
