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寻找治愈方法:COVID-19的潜在小分子治疗方法,第二部分。

Quest for a Cure: Potential Small-Molecule Treatments for COVID-19, Part 2.

作者信息

Hughes David L

机构信息

sp3 Pharma Consulting, 6755 Mira Mesa Boulevard, STE123-217, San Diego, California 92121, United States.

出版信息

Org Process Res Dev. 2021 Apr 19;25(5):1089-1111. doi: 10.1021/acs.oprd.1c00100. eCollection 2021 May 21.

Abstract

During the first year of the outbreak of the COVID-19 pandemic, many drugs and drug candidates have been evaluated as treatment options. None yet has proved to be an effective cure, but progress in controlling the disease has been made. In June 2020 we published an article that described the mechanistic rationale behind the repurposing of seven licensed drugs in clinical trials for the treatment of COVID-19 and reviewed synthetic routes to these drugs. Several developments have occurred since then. Remdesivir (trade name Veklury) has been approved for use in the U.S. and Europe. Dexamethasone, a steroid drug first approved in 1959, has shown mortality reduction in severe COVID patients. Molnupiravir, a new and promising oral antiviral drug, is being studied in late-stage clinical trials. In this review, we update synthetic work that has been recently published on remdesivir, provide an overview of several routes to molnupiravir, and review classical routes to dexamethasone as well as some of those more recently developed.

摘要

在新冠疫情爆发的第一年,许多药物及候选药物已被评估为治疗选项。目前尚无药物被证明是有效的治愈方法,但在控制该疾病方面已取得进展。2020年6月,我们发表了一篇文章,阐述了七种已获许可药物在治疗新冠病毒病临床试验中重新利用的作用机制原理,并回顾了这些药物的合成路线。自那时以来又有了一些新进展。瑞德西韦(商品名:Veklury)已在美国和欧洲获批使用。地塞米松,一种1959年首次获批的甾体药物,已显示可降低重症新冠患者的死亡率。莫努匹韦,一种新型且有前景的口服抗病毒药物,正在进行后期临床试验研究。在这篇综述中,我们更新了最近发表的关于瑞德西韦的合成研究工作,概述了莫努匹韦的几种合成路线,并回顾了地塞米松的经典合成路线以及一些最近开发的合成路线。

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