Patent evaluation of WO2019209182 (A1) 2019-10-31 (Conjugated Oligoelectrolytes as Antimicrobial Agents)

ABSTRACT

Introduction

The insurgence of antibiotic resistance represents one of the biggest public health challenges of our times. During the years, different compounds were developed to fight against resistant bacterial cells, exploiting different mechanisms of action.

Areas covered

The patent application describes a set of antimicrobial compounds bearing to the class of the conjugated oligoelectrolytes (COEs). These are molecules characterized by hydrophobic conjugated backbone and terminal polar ionic pendants, able to intercalate into lipid bilayers of bacterial cells. The patent reports the preparation of 15 new compounds and the evaluation of their antimicrobial effect against ESKAPE pathogens (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterobacter spp.).

Expert opinion

The preparation of the compounds claimed is simple and the preliminary activity data are very interesting. Among the claimed compounds, COE-D8, COE-T42, and COE-T62 have the ability to strongly inhibit the bacterial growth at doses similar to the ones of last resource antibiotics. Unfortunately, no in-vivo data are reported. Moreover, the presence of several quaternary amines limits the potential application of these compounds only to topical uses.

KEYWORDS:

• Antibiotic resistance
• conjugated oligoelectrolytes
• ESKAPE pathogens
• microbial membranes

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This paper has not been funded.