Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123, Palermo, Italy.
Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123, Palermo, Italy.
Eur J Med Chem. 2023 Mar 5;249:115136. doi: 10.1016/j.ejmech.2023.115136. Epub 2023 Jan 20.
Viruses have been recognized as the etiological agents responsible for many pathological conditions ranging from asymptomatic infections to serious diseases, even leading to death. For this reason, many efforts have been made to identify selective viral targets with the aim of developing efficient therapeutic strategies, devoid of drug-resistance issues. Considering their crucial role in the viral life cycle, polymerases are very attractive targets. Among the classes of compounds explored as viral polymerases inhibitors, here we present an overview of non-nucleoside triazole-based compounds identified in the last fifteen years. Furthermore, the structure-activity relationships (SAR) of the different chemical entities are described in order to highlight the key chemical features required for the development of effective antiviral agents.
病毒已被确认为引起许多病理状况的病原体,这些状况的范围从无症状感染到严重疾病,甚至导致死亡。出于这个原因,人们已经做出了许多努力来识别具有选择性的病毒靶标,目的是开发有效的治疗策略,而没有耐药性问题。考虑到它们在病毒生命周期中的关键作用,聚合酶是非常有吸引力的靶标。在作为病毒聚合酶抑制剂探索的化合物类别中,我们在此概述了过去十五年中发现的基于非核苷三唑的化合物。此外,还描述了不同化学实体的结构-活性关系(SAR),以突出开发有效抗病毒药物所需的关键化学特征。