A concise synthesis and evaluation of new malonamide derivatives as potential α-glucosidase inhibitors

• A series of new malonamide derivatives were synthesized.
• In vitro inhibition against α-glucosidase enzyme was evaluated.
• 4K (IC50 = 11.7 ± 0.5 μM) identified as a potent α-glucosidase inhibitor compared to acarbose (IC50 = 840 ± 1.73 μM), in vitro.
• Cytotoxicity of 4a–4m were also evaluated against a number of cancer and normal cell lines.

A series of new malonamide derivatives were synthesized by Michael addition reaction of N1,N3-di(pyridin-2-yl)malonamide into α,β-unsaturated ketones mediated by DBU in DCM at ambient temperature. The inhibitory potential of these compounds in vitro, against α-glucosidase enzyme was evaluated. Result showed that most of malonamide derivatives were identified as a potent inhibitors of α-glucosidase enzyme. Among all the compounds, 4K (IC50 = 11.7 ± 0.5 μM) was found out as the most active one compared to standard drug acarbose (IC50 = 840 ± 1.73 μM). Further cytotoxicity of 4a–4m were also evaluated against a number of cancer and normal cell lines and interesting results were obtained.

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