Novel Thiazolone-Benzenesulphonamide Inhibitors of Human and Bacterial Carbonic Anhydrases
Journal of Enzyme Inhibition and Medicinal Chemistry 2023
Morteza Abdoli, Viviana De Luca, Clemente Capasso, Claudiu T. Supuran, Raivis Žalubovskis

A small library of novel thiazolone-benzenesulphonamides has been prepared and evaluated for their ability to inhibit three human cytosolic carbonic anhydrases (hCA I, hCA II, and hCA VII) and three bacterial carbonic anhydrases (MscCAβ, StCA1, and StCA2). All investigated hCAs were inhibited by the prepared compounds 4a–4j in the low nanomolar range. These compounds were effective hCA I inhibitors (KIs of 31.5–637.3 nM) and excellent hCA II (KIs in the range of 1.3–13.7 nM) and hCA VII inhibitors (KIs in the range of 0.9–14.6 nM). The most active analog in the series, 4-((4-oxo-5-propyl-4,5-dihydrothiazol-2-yl)amino)benzenesulphonamide 4d, strongly inhibited bacterial MscCAβ, with KI of 73.6 nM, considerably better than AAZ (KI of 625 nM). The tested compounds displayed medium inhibitory potency against StCA1 (KIs of 69.2–163.3 nM) when compared to the standard drug (KI of 59 nM). However, StCA2 was poorly inhibited by the sulphonamides reported here, with KIs in the micromolar range between 275.2 and 4875.0 nM.


Atslēgas vārdi
Carbonic anhydrase inhibitors | Mammaliicoccus (Staphylococcus) sciuri | Salmonella enterica (serovar Typhimurium) | sulphonamides | thiazolones
DOI
10.1080/14756366.2022.2163243
Hipersaite
https://www.tandfonline.com/doi/full/10.1080/14756366.2022.2163243

Abdoli, M., De Luca, V., Capasso, C., Supuran, C., Žalubovskis, R. Novel Thiazolone-Benzenesulphonamide Inhibitors of Human and Bacterial Carbonic Anhydrases. Journal of Enzyme Inhibition and Medicinal Chemistry, 2023, Vol. 38, No. 1, Article number 2163243. ISSN 1475-6366. e-ISSN 1475-6374. Available from: doi:10.1080/14756366.2022.2163243

Publikācijas valoda
English (en)
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