The catastrophic SARS-CoV-2 outbreak of 2019 has resulted in 235 million confirmed cases of COVID-19 causing >5.2 million deaths globally as of December 2021. SARS-CoV-2 is a highly infectious, RNA beta-coronavirus that can cause life-threatening viral pneumonia in the most serious cases[1]. Although effective COVID-19 vaccines have been developed within unprecedented timelines, a large number of people are either unable due to preexisting medical conditions or unwilling to be vaccinated, and global access challenges remain. Oral SARS-CoV-2-specific therapeutics are urgently needed to prevent more severe disease, hospitalization, and death. In December 2021, Pfrizer's COVID-19 new drug Paxlovid and Merck's COVID-19 new drug Molnupiravir were received emergency authorization from U.S. FDA for use in high-risk patients. And in January 2022, SHIONOGI's 3CLpro inhibitor S-217622 was disclosed with its structure and positive clinical results[2-7].
A series of building blocks will be used as molecular fragments in the design of COVID-19 new drugs
[1] Science (2021), 374(6575), 1586-1593. [2] Chemical Communications (2020), 56(87), 13363-13364. [3] Organic Process Research & Development (2021), 25(12), 2679-2685. [4] WO2021/250648 A1. [5] Chemical & Engineering News (2021), 99(13), 7. [6] Journal of Medicinal Chemistry 2020, 63, 21, 12725-12747. [7] Journal of Medicinal Chemistry (2017), 60(5), 1648-1661.
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