2. Academic Validation
  3. Design, synthesis, biological evaluation, and docking study of new triazole-phenylacetamide derivatives as α-glucosidase inhibitors

Design, synthesis, biological evaluation, and docking study of new triazole-phenylacetamide derivatives as α-glucosidase inhibitors

  • Bioorg Chem. 2023 Sep 6:141:106844. doi: 10.1016/j.bioorg.2023.106844.
Shuang Luo 1,  Wei Yang 1,  Yong Huang 2,  Zhiyun Peng 3,  Guangcheng Wang 4
Affiliations

Affiliations

  • 1 State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, China; School of Pharmacy, Guizhou Medical University, Guiyang, China.
  • 2 Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang, China.
  • 3 Clinical Trails Center, The Affiliated Hospital of Guizhou Medical University, Guiyang, China. Electronic address: pengzhiyun1986@163.com.
  • 4 State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, China. Electronic address: wanggch123@163.com.
PMID: 37703743 DOI: 10.1016/j.bioorg.2023.106844
Abstract

To discover potent α-glucosidase inhibitors, a class of novel triazole-phenylacetamide derivatives (5a-5p) were designed, prepared, and tested for their α-glucosidase inhibitory effects. All tested compounds (5a-5p) displayed a strong α-glucosidase inhibitory activity (IC50 = 6.69 ± 0.18-113.65 ± 2.94 μM) in comparison with the positive control acarbose (IC50 = 723.06 ± 11.26 μM). Thereinto, 5g (IC50 = 6.69 ± 0.18 μM) showed the best anti-α-glucosidase activity and behaved as a mixed-type inhibitor with the value of Ki and Kis to be 1.65 μM and 4.54 μM, respectively. Besides, fluorescence quenching experiment, three-dimensional fluorescence spectra assay, circular dichroism analysis, and molecular docking studies indicated that 5g may inhibit α-glucosidase activity by binding with its active site as well as changing the secondary structure of α-glucosidase. Combined with the inhibition effect on the rise of postprandial blood glucose level and low cytotoxicity of 5g, it could be concluded that these title compounds may play a role as lead compounds to develop novel α-glucosidase inhibitors.

Keywords

Phenylacetamide; T2DM; Triazole; α-Glucosidase inhibitor.

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