Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 25, Issue 20, Pages 4567-4571Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.08.059
Keywords
alpha-Glucosidase inhibitors; Prenyl; Geranyl; Flavonoid; Docking study
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Funding
- International Science & Technology Cooperation Program of China [2013DFA31160]
- Scientific Research Foundation of Tianjin University of Science Technology [20110115]
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Three series of prenylated and/or geranylated flavonoids were synthesized and evaluated for their alpha-glucosidase inhibitory activity. The 3',5'-digeranylated chalcone (16) was identified as a new alpha-glucosidase inhibitor whose activity (IC50 = 0.90 mu M) was 50-fold more than that of acarbose (IC50 = 51.32 mu M). Molecular docking studies revealed the existence of strong hydrophobic interaction and H-bonding between compound 16 and alpha-glucosidase's active site. The inhibitory mode analysis showed that 16 exhibited a competitive inhibitory mode. (C) 2015 Elsevier Ltd. All rights reserved.
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