Abstract

Thousands of phenolic derivatives have been identified in the plant kingdom, which exert crucial roles in plant physiology. Many such derivatives were shown to produce pharmacological effects in humans which address their use in medicine as antiaging, anti-inflammatory, antioxidant, antidiabetic, and antiproliferative agents among others. Numerous such pharmacological activities are likely to derive from the inhibition of human carbonic anhydrase (CAs, EC 4.2.1.1) isoforms. Phenols, in fact, are able to anchor to the zinc-bound nucleophile present in the enzyme active site, blocking the catalytic action of CAs in humans and/or encoded in various microorganisms. This chapter discusses natural, semisynthetic and synthetic phenol derivatives that exhibited a CA inhibitory action. The discussion over the CA inhibition profiles is categorized as the inhibition of human CAs and inhibition of CAs from microorganisms. Multiple types of inhibition mechanisms by phenolic derivatives are discussed according to X-ray crystallographic resolutions and in silico studies.