β-Lactamase inhibitors: a survey of the patent literature 2000 – 2004

Abstract

The increasing incidence of drug-resistant pathogenic bacteria due to the emergence of different classes of β-lactamases continues to serve as an impetus for efforts directed at improving formulation and chemical processes of existing inhibitors, and discovery of novel inhibitors. This review summarises patent disclosures on β-lactamase inhibitors published during the period January 2000 to December 2004. Several patent disclosures describing novel pharmaceutical formulations, chemical and biosynthetic processes for the clinically useful inhibitors, namely clavulanic acid, tazobactam and sulbactam, are selected for review. Furthermore, patents on novel β-lactam-based and non-β-lactam-based compounds as potential inhibitors of serine β-lactamases and metallo-β-lactamases detailing their chemistry and biological evaluation are also reviewed.

Keywords::

• β-lactam antibiotic
• β-lactamase
• β-lactamase inhibitor
• carbacephem
• carbapenem
• clavulanic acid
• metallo-β-lactamase
• penam sulfone
• penem
• oxapenem
• sulbactam
• tazobactam

Acknowledgement

The author would like to thank the Faculty of Pharmacy, Kuwait University, for providing the facilities used during preparation of the manuscript.