LAUSR

Aldose reductase (AR) is the first and rate‐limiting enzyme of the polyol pathway, which converts glucose to sorbitol in an NADPH‐dependent reaction. α‐Glycosidase breaks down starch and disaccharides to glucose. Hence, inhibition of these enzymes can be regarded a considerable approach in the treatment of diabetic complications. AR was purified from sheep liver using simple chromatographic methods. The inhibitory effects of pyrazolyl–thiazoles ((3aR,4S,7R,7aS)‐2‐(4‐{1‐[4‐(4‐bromophenyl)thiazol‐2‐yl]‐5‐(aryl)‐4,5‐dihydro‐1H‐pyrazol‐3‐yl}phenyl)‐3a,4,7,7a‐tetrahydro‐1H‐4,7‐methanoisoindole‐1,3(2H)‐dione derivatives; 3a–i) on AR and α‐glycosidase enzymes were investigated. All compounds showed a good inhibitory action against AR and α‐glycosidase. Among these compounds, compound 3d exhibited the best inhibition profiles against AR, with a Ki value of 7.09 ± 0.19 µM, whereas compound 3e showed the lowest inhibition effects, with a Ki value of 21.89 ± 1.87 µM. Also, all compounds showed efficient inhibition profiles against α‐glycosidase, with Ki values in the range of 0.43 ± 0.06 to 2.30 ± 0.48 µM, whereas the Ki value of acarbose was 12.60 ± 0.78 µM. Lastly, molecular modeling approaches were implemented to predict the binding affinities of compounds against AR and α‐glycosidase. In addition, the ADME analysis of the molecules was performed.