Background

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.

Technology Overview

Researchers at the University of Hawai‘i and Florida International University have developed novel inhibitors of bacterial topoisomerase I that have activity against gram-positive and -negative bacteria. They have synthesized fluoroquinophenoxazine analogs and demonstrated their activities as topoisomerase I inhibitors and antibacterial agents.

Further Details:

Synthesis, evaluation, and CoMFA study of fluoroquinophenoxazine derivatives as bacterial topoisomerase IA inhibitors”, Eur J Med Chemistry, 2017 Jan 5; 125: 515-527.

Benefits

A mechanism of action distinct from commercially available antibiotics
Potential treatment option for multi-drug resistant (MDR) bacterial pathogens that are resistant to currently available antibiotics
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

Applications

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 E. 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)

Opportunity

Seeking a business partner to develop and commercialize novel inhibitors of bacterial topoisomerase I that have activity against gram-positive and -negative bacteria.

Bacterial Topoisomerase I Inhibitors with Antibacterial Activity

Patents

IP Status

Seeking