Trifluoromethylpyridines in Drug DiscoveryTrifluoromethylpyridine fragment exists in at least three marketed drugs: Agios’ isocitrate dehydrogenase 2 (IDH2) allosteric inhibitor enasidenib (Idhifa), Upjohn’s HIV protease inhibitor tipranavir, and Janssen’s androgen receptor antagonist apalutamide. The trifluoromethyl group may form tetrel bonding with heteroatoms on target proteins and the nitrogen atom on pyridine can serve as ahydrogen bond acceptor, establishing further binding points to target proteins. As a consequence, trifluoromethylpyridine is a privileged structure in drug discovery. It may offer tighter binding to the target protein, improving a drug’s solubility, metabolism, stability, and other drug-like properties.
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