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Amine- and Amino Acid-Based Compounds as Carbonic Anhydrase Activators

Andrea Angeli^1,2, Emanuela Berrino³, Simone Carradori⁴

¹NEUROFARBA Department, Pharmaceutical and Nutraceutical Section, University of Florence, via Ugo Schiff 6, 50019 Sesto Fiorentino, FI, Italy.

Molecules (Basel, Switzerland)

|December 10, 2021

Abstract:

After being rather neglected as a research field in the past, carbonic anhydrase activators (CAAs) were undoubtedly demonstrated to be useful in diverse pharmaceutical and industrial applications. They also improved the knowledge of the requirements to selectively interact with a CA isoform over the others and confirmed the catalytic mechanism of this class of compounds. Amino acid and amine derivatives were the most explored in in vitro, in vivo and crystallographic studies as CAAs. Most of them were able to activate human or non-human CA isoforms in the nanomolar range, being proposed as therapeutic and industrial tools. Some isoforms are better activated by amino acids than amines derivatives and the stereochemistry may exert a role. Finally, non-human CAs have been very recently tested for activation studies, paving the way to innovative industrial and environmental applications.

Keywords:

activators amine amino acid carbonic anhydrase coral fungi isoform selectivity learning and cognitive impairment neurodegenerative diseases protozoa

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