TY  - JOUR
TI  - Investigation of 1,2,4-Triazole Derivatives as Potantial Anti-Diabetic Agents: In vitro Enzyme Inhibition and In silico Pharmacokinetic Studies
AB  - Diabetes mellitus (DM) is a metabolic disease that causes an increase in blood glucose levels, leading to postprandial hyperglycemia and numerous secondary problems, such as kidney failure, blindness, cardiovascular diseases, and nerve damage. Inhibitors of α amylase and α glucosidase are widely used in the treatment of type-II DM because they can inhibit the digestion of starch. In this study, the inhibition potentials of previously synthesized fluorine-containing 1,2,4-triazole-5-one derivatives (4a-d, 6a-b, 7a-b, 8a-b) were screened against α-amylase and α-glucosidase activities. All the compounds exhibited varying degrees of α- amylase inhibitory potential, ranging from 185.2 ± 3.4 to 535.6 ± 5.5 μM. For α-glucosidase, the IC50 values ranged from 202.1 ± 3.8 to 803.2 ± 10.3 μM, compared to the positive control acarbose (IC50 = 411.3 ± 6.4 μM for α-amylase and IC50 = 252.0 ± 4.8 μM for α-glucosidase). 4c exhibited excellent inhibitory potential in both cases, and we evaluated the mode of inhibition of α-amylase and α-glucosidase through kinetic studies. Furthermore, we calculated the physicochemical and pharmacokinetic properties of molecule 4c using SwissADME software. The results of our research suggest that compound 4c may be a promising candidate for the treatment of type-II DM.
AU  - Öz Tuncay, Fulya
AU  - cakmak, ummuhan
DO  - 10.18185/erzifbed.1216717
PY  - 2023
JO  - Erzincan Üniversitesi Fen Bilimleri Enstitüsü Dergisi
VL  - 16
IS  - 2
SN  - 1307-9085
SP  - 345
EP  - 356
DB  - TRDizin
UR  - http://search/yayin/detay/1195647
ER  -