Anti-infective carbonic anhydrase inhibitors: a patent and literature review.

INTRODUCTION: All microorganisms that cause diseases or illnesses to their host are defined as pathogens. In this paper we will review the current state of the art for inhibiting parasite carbonic anhydrases (CAs, EC 4.2.1.1) with a goal of developing antibacterial, antifungal or antiprotozoan agents possessing a different mechanism of action compared with the clinically used drugs to which a considerable degree of drug resistance has been reported.

AREAS COVERED: Cloning of the genomes of many pathogenic microorganisms offered the possibility of exploring alternative pathways for inhibiting virulence factors or proteins essential for their life cycle, and such an approach was applied systematically for CAs from prokaryotic and eukaryotic microorganisms. Investigations of CAs in bacteria, fungi and protozoa domains will undoubtedly reveal novel aspects of microbial virulence, these efforts being part of a more general approach of using metalloenzyme inhibitors for designing novel classes of anti-infectives.

EXPERT OPINION: Covers an overview of the patent literature in the field of the anti-infective CA inhibitors. Most of the patents deal with sulfonamide CA inhibitors. Bacterial/fungal/protozoan CAs represent at this moment very promising targets for obtaining anti-infectives devoid of the resistance problems of the clinically used such agents but further studies are needed to validate these and other less investigated enzymes as novel drug targets.