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

Bioorganic & Medicinal Chemistry
2016.0

Abstract

A series of new malonamide derivatives were synthesized by Michael addition reaction of N(1),N(3)-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.

DOI： 10.1016/j.bmc.2016.02.037

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