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

Journal Article
Choudhary, Mohammad Shahidul Islam, Assem Barakat, Abdullah M. Al-Majid, Hazem A. Ghabbour, A.F.M. Motiur Rahma, Kulsoom Javaid, Rehan Imad, Sammer Yousuf, M. Iqbal . 2016
Publication Work Type: 
PhD
Tags: 
α-glucosidase inhibitors
Magazine \ Newspaper: 
Bioorganic & Medicinal Chemistry
Publication Abstract: 

A series of new malonamide derivatives were synthesized by Michael addition reaction ofN1,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 4a4m were also evaluated against a number of cancer and normal cell lines and interesting results were obtained.