1,4-二取代-1,2,3-三唑衍生物对基孔肯雅病毒的抗病毒活性评估
Antiviral evaluation of 1,4-disubstituted-1,2,3-triazole derivatives against Chikungunya virus.
作者信息
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
机构信息
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.
出版信息
Future Virol. 2023 Sep;18(13):865-880. doi: 10.2217/fvl-2023-0142. Epub 2023 Oct 25.
AIM
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.
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.
目的
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。
材料与方法
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。
结果
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。
结论
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。
Zotero 插件