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Synthesis and biological evaluation of solithromycin analogs against multidrug resistant pathogens.


ABSTRACT: Novel antibacterial drugs that treat multidrug resistant pathogens are in high demand. We have synthesized analogs of solithromycin using Cu(I)-mediated click chemistry. Evaluation of the analogs using Minimum Inhibitory Concentration (MIC) assays against resistant Staphylococcus aureus, Escherichia coli, and multidrug resistant pathogens Enterococcus faecium and Acinetobacter baumannii showed they possess potencies similar to those of solithromycin, thus demonstrating their potential as future therapeutics to combat the existential threat of multidrug resistant pathogens.

SUBMITTER: Daher SS 

PROVIDER: S-EPMC6487207 | biostudies-literature | 2019 Jun

REPOSITORIES: biostudies-literature

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Synthesis and biological evaluation of solithromycin analogs against multidrug resistant pathogens.

Daher Samer S SS   Jin Xiao X   Patel Jimmy J   Freundlich Joel S JS   Buttaro Bettina B   Andrade Rodrigo B RB  

Bioorganic & medicinal chemistry letters 20190326 11


Novel antibacterial drugs that treat multidrug resistant pathogens are in high demand. We have synthesized analogs of solithromycin using Cu(I)-mediated click chemistry. Evaluation of the analogs using Minimum Inhibitory Concentration (MIC) assays against resistant Staphylococcus aureus, Escherichia coli, and multidrug resistant pathogens Enterococcus faecium and Acinetobacter baumannii showed they possess potencies similar to those of solithromycin, thus demonstrating their potential as future  ...[more]

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