Gepotidacin, a novel first-in-class triazaacenaphthylene topoisomerase II inhibitor, was tested against 85 type strains and clinical isolates of , , , , and in comparison to levofloxacin, moxifloxacin, azithromycin or clindamycin, and tetracycline. Gepotidacin MICs (μg/ml) were 0.125 (), 0.032 (), 2 (), and 8 ( species). Gepotidacin activity was not affected by resistance to fluoroquinolones, tetracyclines, or macrolides in the strains tested. Gepotidacin merits further study for treating infections caused by these organisms.
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http://dx.doi.org/10.1128/AAC.01064-17 | DOI Listing |
Int J Mol Sci
October 2024
Medicines Discovery Institute, Cardiff University, Cardiff CF10 3AT, UK.
One of the challenges for experimental structural biology in the 21st century is to see chemical reactions happen. () DNA gyrase is a type IIA topoisomerase that can create temporary double-stranded DNA breaks to regulate DNA topology. Drugs, such as gepotidacin, zoliflodacin and the quinolone moxifloxacin, can stabilize these normally transient DNA strand breaks and kill bacteria.
View Article and Find Full Text PDFiScience
October 2024
Institut Pasteur, Université Paris Cité, CNRS UMR 3528, Unité de Microbiologie Structurale, 75015 Paris, France.
Expert Opin Ther Pat
June 2024
Neurofarba Department, Pharmaceutical and Nutraceutical Section, University of Florence, Sesto Fiorentino, Italy.
Introduction: is a common sexually transmitted disease connected with extensive drug resistance to many antibiotics. Presently, only expanded spectrum cephalosporins (ceftriaxone and cefixime) and azithromycin remain useful for its management.
Areas Covered: New chemotypes for the classical antibiotic drug target gyrase/topoisomerase IV afforded inhibitors with potent binding to these enzymes, with an inhibition mechanism distinct from that of fluoroquinolones, and thus less prone to mutations.
Antimicrob Agents Chemother
June 2024
The University of Texas Health Science Center at Tyler, Mycobacteria/Nocardia Laboratory, The University of Texas at Tyler School of Medicine, Tyler, Texas, USA.
Novel antimicrobials are needed to treat rising nontuberculous mycobacteria (NTM) infections. Using standard broth microdilution methods, 68 NTM isolates were tested against gepotidacin, a new, first-in-class, oral triazaacenaphthylene bacterial topoisomerase inhibitor. MICs varied (0.
View Article and Find Full Text PDFACS Infect Dis
April 2024
Department of Biochemistry, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, United States.
Antimicrobial resistance is a global threat to human health. Therefore, efforts have been made to develop new antibacterial agents that address this critical medical issue. Gepotidacin is a novel, bactericidal, first-in-class triazaacenaphthylene antibacterial in clinical development.
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