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2000
Volume 21, Issue 13
  • ISSN: 1570-1808
  • E-ISSN: 1875-628X

Abstract

Background

-Glucosidase has a variety of biological functions. A structural model for a potential -glucosidase inhibitor has been proposed in the studies.

Objective

A series f new diaryl derivatives linked through benzimidazole have been randomly and rationally designed, synthesized, and evaluated for their inhibitory activities against -glucosidase (almond). The proposed structural model provides a new strategy for the design of potent -glucosidase inhibitors.

Methods

According to the model, a series of benzimidazole derivatives were designed and synthesized, and their inhibitory activity, K value, inhibitory type, and binding mode analysis (PDB ID: 2J7C) on -glucosidase (almond) were evaluated.

Results

Two compounds and were the best inhibitors with IC values of 7.86 μM and 3.52 μM, respectively. Their K values were calculated to be 9.91 μM and 5.81 μM, respectively.

Conclusion

The SAR analysis suggested that such benzimidazole derivatives might bind to the active site of -glucosidase mainly through hydrogen bonds on -trihydroxyphenol; the additional phenyl ring on the other side towards the solvent-exposed region played a very important role in improving their inhibitory activity against -glucosidase.

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2023-09-26
2025-05-30
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