ABSTRACT β-Lactamase-mediated resistance is a growing threat to the continued use of β-
lactam antibiotics. The use of the β-lactam-based serine-β-lactamase (SBL) inhibitors …

Background The β-lactam antibiotics represent the most successful drug class for treatment
of bacterial infections. Resistance to them, importantly via production of β-lactamases, which …

Resistance to β-lactam antibacterials, importantly via production of β-lactamases, threatens
their widespread use. Bicyclic boronates show promise as clinically useful, dual-action …

Abstract β-Lactams are the most successful antibacterials, yet their use is threatened by
resistance, importantly as caused by β-lactamases. β-Lactamases fall into two mechanistic …

The use of β‐lactamase inhibitors in combination with β‐lactam antibiotics is an emerging
area in drug discovery. This strategy allows the restoration of the therapeutic efficacy of …

Abstract β-Lactamases enable resistance to almost all β-lactam antibiotics. Pioneering work
revealed that acyclic boronic acids can act as 'transition state analogue'inhibitors of …

The bicyclic boronate VNRX-5133 (taniborbactam) is a new type of β-lactamase inhibitor in
clinical development. We report that VNRX-5133 inhibits serine-β-lactamases (SBLs) and …

ABSTRACT β-Lactamases are the most important mechanisms of resistance to the β-lactam
antibacterials. There are two mechanistic classes of β-lactamases: the serine β-lactamases …

ABSTRACT QPX7728 is a new ultrabroad-spectrum inhibitor of serine and metallo-beta-
lactamases (MBLs) from a class of cyclic boronates that gave rise to vaborbactam. The …

Clavulanic acid and avibactam are clinically deployed serine β‐lactamase inhibitors,
important as a defence against antibacterial resistance. Bicyclic boronates are recently …