期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 28, 期 3, 页码 302-309出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.12.048
关键词
Diarylpentanoids; alpha-Glucosidase inhibitory activity; Docking; Polyhydroxyphenyl; Furanyl
资金
- Ministry of Higher Education (MOHE) of Malaysia [FRGS/1/2014/ST01/UPM/02/1 (5538011)]
A series of thirty-four diarylpentanoids derivatives were synthesized and evaluated for their alpha-glucosidase inhibitory activity. Eleven compounds (19, 20, 21, 24, 27, 28, 29, 31, 32, 33 and 34) were found to significantly inhibit alpha-glucosidase in which compounds 28, 31 and 32 demonstrated the highest activity with IC50 values ranging from 14.1 to 15.1 mu M. Structure-activity comparison shows that multiple hydroxy groups are essential for alpha-glucosidase inhibitory activity. Meanwhile, 3,4-dihydroxyphenyl and furanyl moieties were found to be crucial in improving alpha-glucosidase inhibition. Molecular docking analyses further confirmed the critical role of both 3,4-dihydroxyphenyl and furanyl moieties as they bound to alpha-glucosidase active site in different mode. Overall result suggests that diarylpentanoids with both five membered heterocyclic ring and polyhydroxyphenyl moiety could be a new lead design in the search of novel alpha-glucosidase inhibitor. (C) 2017 Elsevier Ltd. All rights reserved.
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