Carbohydrate-modified carbonic anhydrase inhibitors: Advances and challenges

Carbonic anhydrases (CAs) are a family of metalloenzymes that catalyze the reversible conversion of carbon dioxide into bicarbonate and proton, a key reaction involved in numerous physiological and pathological processes. Over the past few decades, CAs have attracted considerable attention as therapeutic targets for conditions such as glaucoma, epilepsy, and cancer. The development of highly potent and selective inhibitors has consequently become a major focus, leading to the identification of novel drug candidates. Among the various strategies explored, the design of carbohydrate-based carbonic anhydrase inhibitors (CAIs) has proven to be particularly versatile for achieving selective CA targeting. The introduction of glycosyl groups as hydrophilic moieties into different CAI frameworks has resulted in the discovery of diverse sugar-based CAIs with significant inhibitory activity. This chapter provides an overview of carbohydrate-based CAIs reported to date.