Abstract
Microbial pathogens are becoming increasingly resistant to
current antibiotics, limiting the availability of clinical treatment options
for bacterial infections. It is imperative to develop novel classes of
antibacterial compounds, preferably against a new target, to avoid
cross-resistance. Clinically, topoisomerase enzymes represent attractive and
successful targets for anticancer and antibacterial chemotherapy. Bacterial
topoisomerase I is a novel topoisomerase target that is essential for the
viability of pathogens including mycobacteria, Helicobacter pylori and
Pseudomonas aeruginosa.Researchers at FIU and the University of Hawai‘i have
synthesized fluoroquinophenoxazine analogs and demonstrated their activities as
topoisomerase I inhibitors and bactericidal antibacterial agents.
Benefit
Offer a mechanism of action distinct from commercially available antibioticsProvide much needed treatment options for multi-drug resistant (MDR) bacterial pathogens that are resistant to currently available antibioticsCan be easily formulated into compositions together with pharmaceutically acceptable carriers for parenteral injection, solid or liquid form oral administration, and rectal administrationExhibit improved solubility characteristics as compared with prior quinolone-3-carboxylic acid compounds
Market Application
Antibacterial drug development through in vitro cytotoxicity against mammalian cells and in vivo animal testingTreatment against bacterial pathogens, including both gram-positive and -negative bacteria such as coli, Staphylococcus aureus, Streptococcus pneumoniae, Helicobacter pylori, Mycobacterium bovis, Mycobacterium africanum, Mycobacterium microti, Mycobacterium canetti, Mycobacterium smegmatis, and Mycobacterium tuberculosisTreatment of infections in the form of biofilms formed by mycobacteria, including tuberculosis (Mtb) and nontuberculous mycobacteria (NTM)
Brochure
