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

作者：Parthiban Valentina; Kaliappan Ilango^*; Chander Subhash; Sankaranarayanan Murugesan

来源：Bioorganic Chemistry, 2017, 74: 158-165.

DOI：10.1016/j.bioorg.2017.07.018

• Antidiabetic
• Molecular docking
• Quercetin
• Indole
• Hyperglycaemia

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.

• 出版日期2017-10