Kocyigit, Umit M.Aslan, Osman NuriGulcin, IlhamiTemel, YusufCeylan, Mustafa2019-07-272019-07-282019-07-272019-07-2820160365-62331521-4184https://dx.doi.org/10.1002/ardp.201600092https://hdl.handle.net/20.500.12418/7099Carbonic anhydrase (CA, EC 4.2.1.1) is a member of the metalloenzyme family. It catalyzes the rapid conversion of carbon dioxide (CO2) and water to bicarbonate (HCO3-) and protons (H+) and also plays an important role in biochemical and physiological processes. In this study, a number of novel 2-(4-(aryl)thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives were synthesized and evaluated for their inhibitory characteristics against the human CA isoenzymes I and II (hCA I and hCA II). The structures of the new molecules 8a-i were confirmed by means of IR, H-1 NMR, C-13 NMR, and elemental analysis. These compounds exhibited excellent inhibitory effects, in the low nanomolar range, with K-i values in the range of 27.07-37.80 nM against hCA I and in the range of 11.80-25.81nM against hCA II. Our findings suggest that the new isoindolylthiazole derivatives have superior inhibitory effect over acetazolamide (AZA), which is used as clinical CA inhibitor with K-i values of 34.50 and 28.93nM against the hCA I and hCA II isoenzymes, respectively.en10.1002/ardp.201600092info:eu-repo/semantics/closedAccessCarbonic anhydraseEnzyme inhibitionIsoindoleThiazoleArticle34912963955278595852-s2.0-85000399323Q2WOS:000392963000007Q2