ZFIN Image: Zorman et al., 2023, Fig. 4

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Figure Caption

Fig. 4 Gradual structural and physicochemical optimizations of different NBTIs showing diminished hERG inhibition, while maintaining excellent antibacterial properties. Overall, more than a 100-fold hERG improvement was achieved after differentially fluorinating the p-halogenated phenyl RHS moieties (Kokot et al., 2021), and by substituting the aminopiperidine linker with more polar linker variant that does not contain a tertiary amine (Kokot et al., 2022). Furthermore, compound 6, exhibits no cardiotoxicity in vivo zebrafish model, and a favorable in vivo efficacy in a neutropenic murine thigh infection model of MRSA (Kokot et al., 2023).

Acknowledgments

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