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Abstract A novel series of 1-azacoumarin derivatives were designed and evaluated for their in vitro α-amylase, α-glucosidase, and DPP-4 enzymes resulting in effective anti-diabetic agents. The research results showed that these compounds had significant inhibitory effects on both α-amylase and α-glucosidase enzymes, respectively. Compound 4 demonstrated the most potency for α-glucosidase and α-amylase activities which was significantly more powerful than the drug Acarbose. Also, compound 4 Exhibits strong inhibitory activity against DPP-4. Investigating the potential of compound 4 to treat diabetes, we evaluated its cytotoxic and antioxidant properties. Our results indicated that it had a highly effective scavenging ability for DPPH. |