Path to overcome antibiotic resistance

Researchers believe they have solved a serious problem faced by the medical community with the most important antibiotics in general use today, the b-lactam family of products: the increasing development of drug resistance.

Antibiotics resistance is caused by the action of a bacterial lactamase enzyme. Fortunately, it can often be overcome by the use of a serine b-lactamase inhibitor in combination with the antibiotic drug. This approach is successfully used already, for example clavulanic acid is used in combination with amoxycillin in the product Augmentin.

On the other hand, various b-lactam drugs are also inactivated by enzymes called metallo-b-lactamases that cannot be overcome by the current range of serine b-lactamase inhibitors. Until recently, there have been no metallo-b-lactamase inhibitors of any kind to protect the drugs from this type of resistance.

Researchers at Oxford University's Department of Chemistry now believe they have found a solution to this problem. They have discovered a new class of inhibitors of class B bacterial lactamases that are responsible for drug resistance in those bacteria.

The researchers claim to have identified a number of potentially useful inhibitor compounds that are mainly perfluoroalkyl derivatives of a-amino acids or a peptide. These can be made by either conventional routes or by a novel method specially developed by the team.

The new metallo-b-lactamase inhibitors should provide an attractive alternative approach to enhancing antibiotic performance and overcoming antibiotic resistance in bacteria.