Title |
In vitro and in silico evaluations of diarylpentanoid series as α-glucosidase inhibitor
|
---|---|
Published in |
Bioorganic & Medicinal Chemistry Letters, December 2017
|
DOI | 10.1016/j.bmcl.2017.12.048 |
Pubmed ID | |
Authors |
Sze Wei Leong, Faridah Abas, Kok Wai Lam, Khatijah Yusoff |
Abstract |
A series of thirty-four diarylpentanoids derivatives were synthesized and evaluated for their α-glucosidase inhibitory activity. Eleven compounds (19, 20, 21, 24, 27, 28, 29, 31, 32, 33 and 34) were found to significantly inhibit α-glucosidase in which compounds 28, 31 and 32 demonstrated the highest activity with IC50 values ranging from 14.1 to 15.1 µM. Structure-activity comparison shows that multiple hydroxy groups are essential for α-glucosidase inhibitory activity. Meanwhile, 3,4-dihydroxyphenyl and furanyl moieties were found to be crucial in improving α-glucosidase inhibition. Molecular docking analyses further confirmed the critical role of both 3,4-dihydroxyphenyl and furanyl moieties as they bound to α-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 α-glucosidase inhibitor. |
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