Design, synthesis and α-amylase inhibitory activity of novel chromone derivatives

Quercetin is one of the naturally occurring polyphenol flavonoid predominantly known for antidiabetic activity. In the present study, by considering the structural requirements, twenty two novel chromone derivatives (5-26) as alpha-amylase inhibitor were designed and subsequently in silico evaluated for drug likeness behavior. Designed compounds were synthesized, characterized by spectral analysis and finally evaluated for the inhibition of alpha-amylase activity by in vitro assay. Tested compounds exhibited significant to weak activity with IC50 range of 12-125 mu M. Among the tested compounds, analogues 5, 8, 12, 13, 15, 17 and 22 exhibited significant human alpha-amylase inhibitory activity with IC50 values <25 mu M, which can be further explored as anti-hyperglycemic agents. Putative binding mode of the significant and least active alpha-amylase inhibitors with the target enzyme was also explored by the docking studies. (C) 2017 Elsevier Inc. All rights reserved.