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Novel potent and selective human Carbonic Anhydrase inhibitors

Novel potent human Carbonic Anhydrase (hCA) inhibitors have been designed and structurally characterized on XRD2. The molecules are sulfonamides incorporating piperazine bioisosteres and act as potent and selective inhibitors on hCA I, II, IV or IX isoforms.

(Ref: Chiaramonte N. et al, Bioorganic Chemistry, xxx(x), xxx-xxx(2019))

The reversible hydration of CO2 is the most important reaction catalysed by Carbonic Anhydrase (CA) enzymes, affecting several important physiological processes such as pH and electrolyte balance. An abnormal activity of these enzymes often leads to pathological effects. In humans, sixteen different isoforms belonging to the α family have been characterized, differing for cellular and tissue distribution, and catalytic activity.
CA inhibitors (CAI) are used in the clinic as diuretics, antiglaucoma and antiepileptic agents, for renal and central nervous system diseases, pain, and cancer treatment, although their use may be strongly limited by side effects, due to poor isoform selectivity. A rational structure-activity relationships study on a novel series of sulfonamides inhibitors incorporating finely tuned piperazine bioisosteres have been conducted to correlate inhibitor structure, enzyme binding modes and isoform selectivity.

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Sulfonamides incorporating piperazine bioisosteres as potent human Carbonic Anhydrase I, II, IV and IX inhibitors,
Niccolò Chiaramonte, Silvia Bua, Andrea Angeli, Marta Ferraroni, Ilaria Picchioni, Gianluca Bartolucci, Laura Braconi, Silvia Dei, Elisabetta Teodori, Claudiu T. Supuran, Maria Novella Romanelli
Bioorganic Chemistry 2019 xxx (x), xxx-xxx, doi: 10.1016/j.bioorg.2019.103130, PDB: 6RG3, 6RG4, 6RHJ, 6RHK

Last Updated on Wednesday, 03 June 2020 12:11