Paul Finn et al (2018): ‘N-Leucinyl Benzenesulfonamides as Structurally Simplified Leucyl-tRNA Synthetase Inhibitors’, “ACS Medicinal Chemistry Letters”

Antibiotics to treat bacterial infections have transformed human health.  However, much in the news in recent years has been the emergence of bacteria resistant to many, and in some cases all, of the currently available drugs. If this threat continues to grow many aspects of modern medicine will simply become impossible. We need antibiotics to treat serious infections like pneumonia but they’re also essential for patients undergoing routine surgery, like hip and knee replacements or removing an appendix. There is thus an urgent need to develop new antibiotics.

This publication describes the discovery of a new class of antibiotics that has the potential to be developed into new treatments for serious drug-resistant infections.  The compounds target a component of the system that bacteria use to produce their proteins.  By shutting down this system, the new compounds prevent bacterial growth.

The work is multi-disciplinary, involving computer scientists, chemists, and microbiologists working as a team to design, synthesize and test the compounds. Importantly, the mechanism of action of the compounds is novel, and so they can be effective against bacteria that are resistant to conventional agents.

The project is currently in the “optimization” phase, where incremental improvements are made to improve the properties of the drugs.  If successful, clinical trials may be possible in the next two to three years.  With very few novel antibacterials currently in the pipeline, the potential impact of this research is significant.

 

DOI: 10.1021/acsmedchemlett.7b00374

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