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Fluorine in Medicinal Chemistry: In Perspective to COVID-19

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ACS OMEGA
卷 7, 期 22, 页码 18206-18212

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AMER CHEMICAL SOC
DOI: 10.1021/acsomega.2c01121

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  1. National Health and Medical Research Council [APP1157440]

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Researchers have made progress in exploring effective and economical anti-COVID-19 drugs, including fluorinated oral drugs. These drugs can be taken orally at home and used after exposure to the SARS-CoV-2 virus or at the first signs of COVID-19.
Over two years into the outbreak of COVID-19, the quest for effective and economical drugs has become starkly clear to reduce the risk of progression of coronavirus disease. A number of drugs have been investigated, and they can be taken orally at home and be used after exposure to SARS-CoV-2 or at the first sign of COVID-19. Fluorinated oral anti-COVID-19 drugs-including Paxlovid, the first oral tablet for the treatment of COVID-19-constitute an important subgroup. Fluorine has been widely used in the pharmaceutical market and can lead to improved selectivity indices, increased lipophilicity, greater metabolic stability, and improved anti-COVID-19 efficacy. In this mini-review, we will give an update on fluorinated anti-COVID-19 drugs by providing the key information and current knowledge of these drugs, including their molecular design, metabolism and pharmacokinetics, and mechanism of action.

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