Synthesis, α-glucosidase inhibition and molecular docking studies of novel thiazolidine-2,4-dione or rhodanine derivatives

A series of novel thiazolidine-2,4-dione or rhodanine derivatives ( , ) were synthesized and evaluated for their α-glucosidase inhibitory activity. The majority of compounds exhibited potent inhibitory activity in the range of 5.44 ± 0.13 to 50.45 ± 0.39 μM, when compared to the standard drug acarbo...

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Bibliographic Details
Published in:MedChemComm 2017-07, Vol.8 (7), p.1477-1484
Main Authors: Wang, Guang-Cheng, Peng, Ya-Ping, Xie, Zhen-Zhen, Wang, Jing, Chen, Ming
Format: Article
Language:English
Subjects:
Chemistry
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Summary:A series of novel thiazolidine-2,4-dione or rhodanine derivatives ( , ) were synthesized and evaluated for their α-glucosidase inhibitory activity. The majority of compounds exhibited potent inhibitory activity in the range of 5.44 ± 0.13 to 50.45 ± 0.39 μM, when compared to the standard drug acarbose (IC = 817.38 ± 6.27 μM). Among the compounds in the series, compounds , , , , and showed potent inhibitory potential with IC values of 20.95 ± 0.21, 16.11 ± 0.19, 7.72 ± 0.16, 7.91 ± 0.17, 6.59 ± 0.15 and 5.44 ± 0.13 μM, respectively. Compound (IC = 5.44 ± 0.13 μM), containing chloro and rhodanine groups at the 2- and 4-positions of the phenyl ring respectively, was found to be the most active compound that inhibits α-glucosidase activity. Furthermore, molecular docking studies were performed to understand the binding interactions between the molecule and enzyme.
ISSN:2040-2503
2040-2511
DOI:10.1039/c7md00173h