Bioactive oxadiazolo-benzodiazepines: synthesis, α amylase inhibition, antioxidant activity, molecular docking and DFT calculation.

Both diastereoisomers 3 and 4 demonstrated superior activity compared to standard drugs. Compound 3 showed potent α-amylase inhibition IC₅₀ = 22.78 µM) compared to Acarbose IC₅₀ = 123 µM). For antioxidant activity, compounds 4 and 3 exhibited strong DPPH scavenging IC₅₀ = 68.16 and 79.50 μM, respectively), outperforming ascorbic acid. Docking studies confirmed favorable binding interactions within the active sites of target enzymes. The synthesized oxadiazolo-benzodiazepines represent promising multifunctional antidiabetic and antioxidant candidates, warranting further pharmacological investigation.