In Vitro Activity of Gepotidacin, a Novel Triazaacenaphthylene Bacterial Topoisomerase Inhibitor, against a Broad Spectrum of Bacterial Pathogens | Zendy

Douglas J. Biedenbach | Zendy; S. Bouchillon | Zendy; Meredith Hackel | Zendy; Linda A. Miller | Zendy; Nicole E. Scangarella-Oman | Zendy; Charles Jakielaszek | Zendy; D.F. Sahm | Zendy

Open Access

In Vitro Activity of Gepotidacin, a Novel Triazaacenaphthylene Bacterial Topoisomerase Inhibitor, against a Broad Spectrum of Bacterial Pathogens

Author(s) -

Douglas J. Biedenbach,

S. Bouchillon,

Meredith Hackel,

Linda A. Miller,

Nicole E. Scangarella-Oman,

Charles Jakielaszek,

D.F. Sahm

Publication year - 2016

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.02820-15

Subject(s) - topoisomerase , in vitro , microbiology and biotechnology , biology , broad spectrum , bacterial protein , bacteria , chemistry , genetics , combinatorial chemistry

Gepotidacin inhibits bacterial DNA replication through a mode different from that of fluoroquinolones. Gepotidacin and comparators were tested by broth and agar dilution against clinical isolates. The in vitro activities of gepotidacin were comparable against methicillin-susceptible and -resistant Staphylococcus aureus (MSSA and MRSA, respectively) isolates (MIC90, 0.5 μg/ml). The gepotidacin MIC90s were as follows (in micrograms per milliliter) for the indicated bacteria: Streptococcus pyogenes, 0.25; Escherichia coli, 2; Moraxella catarrhalis, ≤ 0.06; Streptococcus pneumoniae (0.25), Haemophilus influenzae, 1; Clostridium perfringens, 0.5; and Shigella spp., 1, including levofloxacin-resistant subsets. Gepotidacin warrants further investigation for clinical development.

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