This article is in Chemistry in Australia magazine: Issue June 2024
Author: William Lumb
Image: Nobeastsofierce/Adobe Stock
Queensland researchers are testing compounds that inhibit bacterial resistance to two-thirds of antibiotics prescribed.
The World Health Organization (WHO) has declared antibiotic resistance “one of the biggest threats to global health, food security and development today … Without urgent action we are heading for a post-antibiotic era in which common infections and minor injuries can once again kill”. As part of its 2015 global action plan, WHO recommended “basic research and translational studies to support … new treatments”.
Researchers from the University of Queensland’s School of Chemistry and Molecular Biosciences have taken up the fight to develop a new class of antibiotics. A team led by Professor Gerhard Schenk and Associate Professor Ross McGeary has synthesised compounds that inhibit the enzyme β-lactamase, which bacteria release to destroy β-lactam antibiotics. Two-thirds of all antibiotic prescriptions are β-lactam antibiotics. The novel inhibitors, described in Bioorganic & Medicinal Chemistry Letters (https:// doi.org/10.1016/j.bmcl.2023.129387), act like a shield that protects these antibiotics from a specific class of β-lactamase enzymes known as class B or metallo-β-lactamases (MBL).
Schenk says the team focused on developing MBL inhibitors because “MBLs are enzymes that basically inactivate almost all β-lactam-based antibiotics. The enzymes are also very flexible; in other words, they can mutate quite easily to avoid being inhibited and yet still maintain their activity”. This explains why there are currently no clinically useful MBL inhibitors. Such inhibitors do exist for other β-lactamases (e.g. clavulanic acid is added to the well-known drug Augmentin), but they are only effective against class A, C and D β-lactamases – not class B.
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