一种在体外可中和严重急性呼吸综合征冠状病毒2（SARS-CoV-2）及其最具传染性的变体德尔塔（Delta）和奥密克戎（Omicron）感染的小分子。
A Small Molecule That In Vitro Neutralizes Infection of SARS-CoV-2 and Its Most Infectious Variants, Delta, and Omicron.
作者信息
Reyes-Alcaraz Arfaxad, Qasim Hanan, Merlinsky Elizabeth, Fox Glenn, Islam Tasneem, Medina Bryan, Schwartz Robert J, Craft John W, McConnell Bradley K
机构信息
Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, USA.
Rogers State University, 1701 W. Will Rogers Blvd., Claremore, OK 74017, USA.
出版信息
Biomedicines. 2023 Mar 15;11(3):916. doi: 10.3390/biomedicines11030916.
The COVID-19 pandemic has underscored the urgent need to develop highly potent and safe medications that are complementary to the role of vaccines. Specifically, it has exhibited the need for orally bioavailable broad-spectrum antivirals that are able to be quickly deployed against newly emerging viral pathogens. The Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV2) and its variants Delta and Omicron are still a major threat to patients of all ages. In this brief report, we describe that the small molecule CD04872SC was able to neutralize SARS-CoV2 infection with a half-maximal effective concentration (EC50) = 248 μM. Serendipitously, we also were able to observe that CD04872SC inhibited the infection of the SARS-CoV-2 variants; Delta (EC50 = 152 μM) and Omicron (EC50 = 308 μM). These properties may define CD04872SC as a potential broad-spectrum candidate lead for the development of treatments for COVID-19.
新冠疫情凸显了开发高效且安全的药物的迫切需求，这些药物可作为疫苗的补充。具体而言，这表明需要口服生物利用度高的广谱抗病毒药物，以便能够迅速用于对抗新出现的病毒病原体。严重急性呼吸综合征冠状病毒2（SARS-CoV2）及其变种德尔塔和奥密克戎仍然对各年龄段的患者构成重大威胁。在本简要报告中，我们描述了小分子CD04872SC能够以半数有效浓度（EC50）= 248 μM中和SARS-CoV2感染。意外的是，我们还观察到CD04872SC抑制了SARS-CoV-2变种德尔塔（EC50 = 152 μM）和奥密克戎（EC50 = 308 μM）的感染。这些特性可能使CD04872SC成为开发新冠治疗药物的潜在广谱候选先导物。
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