Biological and Medicinal Chemistry

Fluorine in Medicinal Chemistry: In Perspective to 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—is an important subgroup. Fluorine has been widely used in pharmaceuticals market and can lead to improved selectivity indices, increased lipophilicity, greater metabolic stability, and in this case the 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 chemical structure, drug metabolism and pharmacokinetics, and mechanism of action.


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