FIGURE

Fig. 4

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ZDB-FIG-240305-8

Publication

Zorman et al., 2023 - The overview of development of novel bacterial topoisomerase inhibitors effective against multidrug-resistant bacteria in an academic environment: from early hits to in vivo active antibacterials

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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).

Expression Data

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Antibody Labeling

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Acknowledgments

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