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Drug Design Strategies, Modes of Action, Synthesis and Industrial Challenges Behind Trifluoromethylated New Chemical Entities
Medicinal plants have been an inspiration source for developing new chemical entities,Ìýproviding diverse chemical structures and modes of action for medicinal chemistry strategies.Ìý
Modern medicinal chemistry approaches promote functional group changes to improve NCE’sÌýbiological activity. Incorporating the trifluoromethyl (-CF3) group into organic compounds isÌýcrucial in modern drug design. It may affect the compound's lipophilicity, solubility, stability,Ìýmolecular conformation, and pKa, changes that may lead to the discovery of new medicinesÌýto treat diseases of our times. For this reason, this chemical transformation is currently aÌýhot topic in the organic chemistry field. Chemists are competing to develop better methodsÌýto carry out this transformation efficiently, less hazardously, and cost-effectively. The highÌýnumber of annual scientific publications on trifluoromethylation evidences the competition.Ìý
This review profi les 21 trifluoromethylated New Chemical Entities (NCE) selected in DecemberÌý2020 from the GlobalData database, mainly in late stages of clinical trials (Phase II and III)Ìýor already in the commercial phase, containing one or two -CF3 groups in para or metaÌýpositions of benzene, or a pyridine ring. Synthetic approaches, therapeutic applications, andÌýmanufacturing industrial challenges are provided.
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