Bacterial Topoisomerase I Inhibitors with Antibacterial Activity


Florida International University (FIU) is seeking a business partner to develop and commercialize novel inhibitors of bacterial topoisomerase I that have activity against gram-positive and -negative bacteria.

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.Compound scaffold

  • Antibacterial drug development through in vitro cytotoxicity against mammalian cells and in vivo animal testing
  • Treatment 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 tuberculosis
  • Treatment of infections in the form of biofilms formed by mycobacteria, including tuberculosis (Mtb) and nontuberculous mycobacteria (NTM)
  • Offer a mechanism of action distinct from commercially available antibiotics
  • Provide much needed treatment options for multi-drug resistant (MDR) bacterial pathogens that are resistant to currently available antibiotics
  • Can be easily formulated into compositions together with pharmaceutically acceptable carriers for parenteral injection, solid or liquid form oral administration, and rectal administration
  • Exhibit improved solubility characteristics as compared with prior quinolone-3-carboxylic acid compounds

Call Anne-Laure “Anlo” Schmitt-Olivier at 305-348-5948 or fill out the quick contact form below.