New Thiazolidine-4-Carboxylic Acid Derivatives Act as Promising α-Amylase and α-Glucosidase Inhibitors; Synthesis, In Vitro Pharmacological Evaluation and In Silico Molecular Docking Study

Abstract

The management of diabetes presents difficulties to scientists as this deadly condition continues to affect people worldwide. Diabetes control depends on enzyme inhibition which blocks both α-amylase and α-glucosidase play key roles in the breakdown of carbohydrates after meals.The presented study details potent Thiazolidine-4-Carboxylic Acid Derivatives 5(a-l) which exhibit strong inhibition against α-amylase and α-glucosidase. The bio-assays performed in test tubes showed that these compounds could prevent biological effects. The phenyl ring substituents served as the main focus of a structure-activity relationship analysis performed on all synthesized molecules. Molecular docking studies served to determine how the compounds would bind when placed inside the enzyme active pocket.Compound 5e proved its outstanding potential as a α-amylase inhibitor because its IC50 value reached 24.13µg/ml which surpassed the standard acarbose (IC50=32.27µg/ml). The inhibitory properties of compounds 5f and 5g towards α-glucosidase surpassed acarbose reference levels (IC50=30.45µg/ml) with 22.76 and 25.68 µg/ml IC50 values. The reference inhibitor matched suppression levels of the tested compounds 5a, 5b, 5c, and 5d as these compounds displayed strong inhibitory potential against α-amylase as well as against α-glucosidase enzymes.These designed derivatives show effective potential characteristics which can serve as starting compounds to develop forthcoming therapeutic intervention solutions.