Synthesis And Pharmacological Screening Of Thiadiazole Derivatives As Antidiabetic Agents
Keywords:
Antidiabetic Agents, Alpha-Glucosidase Inhibition, Antioxidant Activity, Cyclization, Diabetes Mellitus, Enzyme Inhibition, Pharmacological Screening, Streptozotocin, Structure-Activity Relationship, Thiadiazole Derivatives, Toxicity, In Vivo StudiesAbstract
Thiadiazole derivatives have emerged as promising candidates in antidiabetic drug development owing to their diverse pharmacological properties and favorable bioavailability. This study focuses on the synthesis of novel 1,3,4-thiadiazole derivatives incorporating Schiff base moieties, designed specifically to enhance inhibitory activity against key enzymes involved in diabetes, such as α-glucosidase. The synthesized compounds were characterized using spectroscopic techniques including NMR and mass spectrometry to confirm their structural integrity. In vitro enzymatic assays demonstrated that several analogues exhibited potent inhibitory effects with IC50 values significantly lower than the standard drug acarbose, indicating superior efficacy. Molecular docking studies were employed to elucidate the binding interactions at the active site of enzymes, supporting the experimental findings. Additionally, pharmacokinetic profiling and cytotoxicity evaluations suggested favorable ADME properties and low toxicity, underscoring the safety potential of these derivatives. Collectively, this integrated approach combining synthesis, biochemical evaluation, and computational modeling provides valuable insights into the design of effective thiadiazole-based antidiabetic agents. These findings contribute to the advancement of novel therapeutic options for diabetes management, warranting further in vivo and clinical investigations to confirm efficacy and safety
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