Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 29, Issue 1, Pages 119-123Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.10.018
Keywords
alpha-Glucosidase; Diabetes mellitus; Chromene; Flavonoids
Categories
Funding
- Russian Foundation for Basic Research [17-03-01158]
- Russian Science Foundation [14-25-00139]
- Russian Federation [SP-595.2018.4]
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Herein we report a study of novel arylchromene derivatives as analogs of naturally occurring flavonoids with prominent alpha-glucosidase inhibitory properties. Novel inhibitors were identified via simple stepwise in silico screening, efficient synthesis, and biological evaluation. It is shown that 2-aryl-4H-chromene core retains pharmacophore properties while being readily available synthetically. A lead compound identified through screening inhibits yeast alpha-glucosidase with IC50 of 62.26 mu M and prevents postprandial hyperglycemia in rats at 2.2 mg/kg dose.
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