New Dual Inhibitors of Bacterial Topoisomerases with Broad-Spectrum Antibacterial Activity and In Vivo Efficacy against Vancomycin-Intermediate Staphylococcus aureus

A new series of dual low nanomolar benzothiazole inhibitors of bacterial DNA gyrase and topoisomerase IV were developed. The resulting compounds show excellent broad-spectrum antibacterial activities against Gram-positive Enterococcus faecalis, Enterococcus faecium and multidrug resistant (MDR) Stap...

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Hauptverfasser:	Durcik, Martina, Cotman, Andrej Emanuel, Toplak, Zan, Mozina, Stefan, Skok, Ziga, Szili, Petra Eva, Czikkely, Marton, Maharramov, Elvin, Vu, Thu Hien, Piras, Maria Vittoria, Zidar, Nace, Ilas, Janez, Zega, Anamarija, Trontelj, Jurij, Pardo, Luis A, Hughes, Diarmaid, Huseby, Douglas, Berruga-Fernández, Tália, Cao, Sha, Simoff, Ivailo, Svensson, Richard, Korol, Sergiy V, Jin, Zhe, Vicente, Francisca, Ramos, Maria C, Mundy, Julia E. A, Maxwell, Anthony, Stevenson, Clare E. M, Lawson, David M, Glinghammar, Bjorn, Sjostrom, Eva, Bohlin, Martin, Oreskar, Joanna, Alver, Sofie, Janssen, Guido V, Sterk, Geert Jan, Kikelj, Danijel, Pal, Csaba, Tomasic, Tihomir, Masic, Lucija Peterlin
Format:	Artikel
Sprache:	eng
Schlagworte:	Infectious Medicine Infektionsmedicin Läkemedelskemi Medicinal Chemistry Microbiology in the medical area Mikrobiologi inom det medicinska området
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Zusammenfassung:	A new series of dual low nanomolar benzothiazole inhibitors of bacterial DNA gyrase and topoisomerase IV were developed. The resulting compounds show excellent broad-spectrum antibacterial activities against Gram-positive Enterococcus faecalis, Enterococcus faecium and multidrug resistant (MDR) Staphylococcus aureus strains [best compound minimal inhibitory concentrations (MICs): range,
DOI:	10.1021/acs.jmedchem.2c01905