Design, Synthesis, Biological Evaluation, and Molecular Docking Studies of Novel 1,3,4-Thiadiazole Derivatives Targeting Both Aldose Reductase and α-Glucosidase for Diabetes Mellitus.

ABSTRACT: We have developed new 1,3,4-thiadiazole derivatives and examined their ability to inhibit aldose reductase and α-glucosidase. All of the members of the series showed a higher potential of aldose reductase inhibition (K _I: 15.39 ± 1.61-176.50 ± 10.69 nM and IC₅₀: 20.16 ± 1.07-175.40 ± 6.97 nM) compared to the reference inhibitor epalrestat (K _I: 837.70 ± 53.87 nM, IC₅₀: 265.00 ± 2.26 nM). Furthermore, compounds 6a, 6g, 6h, 6j, 6o, 6p, and 6q showed significantly higher inhibitory activity (K _I: 4.48 ± 0.25 μM-15.86 ± 0.92 μM and IC₅₀: 4.68 ± 0.23 μM-34.65 ± 1.78 μM) toward α-glucosidase compared to the reference acarbose (K _I: 21.52 ± 2.72

SUBMITTER: Kaya B 

PROVIDER: S-EPMC12079242 | biostudies-literature | 2025 May

REPOSITORIES: biostudies-literature