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Synthesis, Biological Evaluation, and Molecular Docking Studies of Novel Isatin-Thiazole Derivatives as ?-Glucosidase Inhibitors.

ABSTRACT: A series of novel isatin-thiazole derivatives were synthesized and screened for their in vitro ?-glucosidase inhibitory activity. These compounds displayed a varying degree of ?-glucosidase inhibitory activity with IC50 ranging from 5.36 ± 0.13 to 35.76 ± 0.31 ?m as compared to the standard drug acarbose (IC50 = 817.38 ± 6.27 ?m). Among the series, compound 6p bearing a hydroxyl group at the 4-position of the right phenyl and 2-fluorobenzyl substituent at the N1-positions of the 5-methylisatin displayed the highest inhibitory activity with an IC50 value of 5.36 ± 0.13 ?m. Molecular docking studies revealed the existence of hydrophobic interaction, CH-? interaction, arene-anion interaction, arene-cation interaction, and hydrogen bond between these compounds and ?-glucosidase enzyme.

SUBMITTER: Xie Z

PROVIDER: S-EPMC6154535 | biostudies-literature | 2017 Apr

REPOSITORIES: biostudies-literature

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Synthesis, Biological Evaluation, and Molecular Docking Studies of Novel Isatin-Thiazole Derivatives as α-Glucosidase Inhibitors.

Xie Zhenzhen Z Wang Guangcheng G Wang Jing J Chen Ming M Peng Yaping Y Li Luyao L Deng Bing B Chen Shan S Li Wenbiao W

Molecules (Basel, Switzerland) 20170420 4

A series of novel isatin-thiazole derivatives were synthesized and screened for their in vitro α-glucosidase inhibitory activity. These compounds displayed a varying degree of α-glucosidase inhibitory activity with IC50 ranging from 5.36 ± 0.13 to 35.76 ± 0.31 μm as compared to the standard drug acarbose (IC50 = 817.38 ± 6.27 μm). Among the series, compound 6p bearing a hydroxyl group at the 4-position of the right phenyl and 2-fluorobenzyl substituent at the N</i ...[more]

PMID: 28425975

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