This study synthesized a novel series of ~55 Benzodioxol derivatives and evaluated their multitarget biological activities. In vitro and in vivo assays assessed their effects on AMPA receptors, COX enzymes, α-amylase, and cancer cell lines. Key findings revealed potent AMPA receptor modulation, suggesting therapeutic potential for Parkinson’s disease. Aryl acetate derivatives showed strong COX-2 inhibition, while select acetic acid and carboxamide compounds exhibited superior α-amylase inhibition, outperforming Acarbose in reducing blood sugar levels. Molecular docking studies clarified binding interactions with AMPA receptors and α-amylase, while bioavailability predictions (Molinspiration, Lipinski’s rule of five) aligned with experimental data. Overall, this work identifies promising candidates for neurological disorders, NSAID development, and diabetes treatment.
