Matyugina E S, Novikov M S, Kozlovskaya L I, Volok V P, Shustova E Y, Ishmukhametov A A, Kochetkov S N, Khandazhinskaya A L
Engelhardt Institute of Molecular Biology, Moscow, 119991 Russia.
Volgograd State Medical University, Volgograd, 400131 Russia.
Acta Naturae. 2021 Oct-Dec;13(4):78-81. doi: 10.32607/actanaturae.11479.
The pandemic caused by the novel betacoronavirus SARS-CoV-2 has already claimed more than 3.5 million lives. Despite the development and use of anti-COVID-19 vaccines, the disease remains a major public health challenge throughout the world. Large-scale screening of the drugs already approved for the treatment of other viral, bacterial, and parasitic infections, as well as autoimmune, oncological, and other diseases is currently underway as part of their repurposing for development of effective therapeutic agents against SARS-CoV-2. In this work, we present the results of a phenotypic screening of libraries of modified heterocyclic bases and 5'-norcarbocyclic nucleoside analogs previously synthesized by us. We identified two leading compounds with apparent potential to inhibit SARS-CoV-2 replication and EC values in a range of 20-70 μM. The structures of these compounds can be further optimized to develop an antiviral drug.
由新型β冠状病毒SARS-CoV-2引发的大流行已导致超过350万人死亡。尽管已研发并使用了抗COVID-19疫苗，但该疾病仍是全球主要的公共卫生挑战。目前正在对已批准用于治疗其他病毒、细菌和寄生虫感染以及自身免疫性、肿瘤性和其他疾病的药物进行大规模筛选，作为将其重新用于开发抗SARS-CoV-2有效治疗剂的一部分。在这项工作中，我们展示了对我们之前合成的修饰杂环碱基库和5'-去碳环核苷类似物进行表型筛选的结果。我们鉴定出两种具有明显抑制SARS-CoV-2复制潜力且半数有效浓度（EC）值在20-70μM范围内的先导化合物。这些化合物的结构可进一步优化以开发抗病毒药物。
