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.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5610498PMC
http://dx.doi.org/10.1128/AAC.01064-17DOI Listing

Publication Analysis

Top Keywords

activities gepotidacin
4
gepotidacin gsk2140944
4
gsk2140944 antimicrobial
4
antimicrobial agents
4
agents human
4
human mycoplasmas
4
mycoplasmas ureaplasmas
4
gepotidacin
4
ureaplasmas gepotidacin
4
gepotidacin novel
4

Similar Publications

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 PDF

Molecular mechanism of a triazole-containing inhibitor of DNA gyrase.

iScience

October 2024

Institut Pasteur, Université Paris Cité, CNRS UMR 3528, Unité de Microbiologie Structurale, 75015 Paris, France.

Article Synopsis
  • * Researchers synthesized triazole-containing compounds that showed strong antibacterial effects, especially one named BDM71403, which was found to be more effective than the reference drug, gepotidacin.
  • * Detailed structural studies using cryo-electron microscopy revealed how BDM71403 interacts with DNA gyrase and DNA, providing insights for future antibiotic development to combat resistant bacteria.
View Article and Find Full Text PDF

Management of infection: from drug resistance to drug repurposing.

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.

View Article and Find Full Text PDF

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 PDF

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.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!