Abstract
About one-fifth of the currently marketed pharmaceuticals are organofluorine compounds. Some of the top-selling drugs such as atorvastatin, Crestor, efavirenz, fluoxetine, Ciprobay, fluticasone propionate, Faslodex, ezetimibe, Celebrex, and sitagliptin consist of a fluoroaryl moiety, a gem-difluoromethylene moiety, or a trifluoromethyl moiety. Fluoxetine, a serotonin reuptake inhibitor is a widely used antidepressant drug. Fluorinated drugs such as atorvastatin and ezetimibe are among the top-selling antihypercholesterolemia drugs. Antibacterials, such as flurithromycin have enhanced bioavailability and metabolic stability due to the presence of a fluorine substituent at the metabolically vulnerable site. Mefloquine, a trifluoromethyl-substituted quinine analog, is one of the most successful drugs for treating malaria. This chapter outlines the synthesis and mechanisms of action of fluorinated drugs focusing on the widely used therapeutics, which include antibacterials, antimalarials, antidiabetics, antiinflammatory agents, antihypercholesterolemia drugs, and antiviral drugs.
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