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Fig. 5 S. aureus DNA gyrase inhibitory activity and cLogP values of a series of aminopiperidine-naphthyridine NBTIs with substituted phenyl RHS moieties (Kolarič et al., 2021; Kolarič et al., 2021; Kokot et al., 2021). Antibacterial activity is enhanced as we move down the halogen group, from fluorine to bromine, as expected for increase in the halogen-bonding enthalpy. Differential fluorination of the RHS moiety enhances on-target inhibitory potency even further. Despite very similar cLogP values, m-difluorinated show higher antibacterial activity compared to m,o-difluorinated ones.
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Full text @ Eur. J. Pharm. Sci.