Download MendeleyTetrazole Is a Novel Zinc Binder Chemotype for Carbonic Anhydrase Inhibition.
Giovannuzzi, S., Angeli, A., Begines, P., Ferraroni, M., Nocentini, A., Supuran, C.T.(2025) ACS Med Chem Lett 16: 163-166
- PubMed: 39811134
- DOI: https://doi.org/10.1021/acsmedchemlett.4c00562
- Primary Citation of Related Structures:
9GU7, 9GUM, 9GUO - PubMed Abstract:
The tetrazole group is here proposed as a zinc-binding warhead for the inhibition of the metalloenzyme carbonic anhydrases. A set of synthesized derivatives incorporating the tetrazole moiety were evaluated as inhibitors against a panel of human isoforms, exhibiting K I values spanning between the submicromolar and low-to-medium micromolar ranges (0.62-19.6 μM). X-ray crystallographic studies were conducted to gain insights into their modes of binding to the target enzyme. These findings mark a significant advancement in the search for inhibitory chemotypes other than classical sulfonamides.
Organizational Affiliation:
NEUROFARBA Department, Section of Pharmaceutical Science, University of Florence, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy.
