IMAGE

Fig. 4

ID: ZDB-IMAGE-240305-7
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
All Figures: Figures for Zorman et al., 2023

Image

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

This image is the copyrighted work of the attributed author or publisher, and ZFIN has permission only to display this image to its users. Additional permissions should be obtained from the applicable author or publisher of the image. Full text @ Eur. J. Pharm. Sci.