New phthalimide-benzamide-1,2,3-triazole hybrids; design, synthesis, α-glucosidase inhibition assay, and docking study

被引:0
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作者
Seyed Esmaeil Sadat-Ebrahimi
Abbas Rahmani
Maryam Mohammadi-Khanaposhtani
Negar jafari
Somayeh Mojtabavi
Mohammad Ali Faramarzi
Mehdi Emadi
Azadeh Yahya-Meymandi
Bagher Larijani
Mahmoud Biglar
Mohammad Mahdavi
机构
[1] Tehran University of Medical Sciences,Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center
[2] Babol University of Medical Sciences,Cellular and Molecular Biology Research Center, Health Research Institute
[3] University of Kansas,Department of Pharmaceutical Chemistry٫ Faculty of pharmacy
[4] Tehran University of Medical Sciences,Department of Pharmaceutical Biotechnology, Faculty of Pharmacy and Biotechnology Research Center
[5] Babol Noshirvani University of Technology,Electrical and Computer Engineering Department
[6] University of Birjand,Department of Chemistry, Faculty of Science
[7] Tehran University of Medical Sciences,Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute
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关键词
Phthalimide; Benzamide; 1,2,3-Triazole; Hybrid; -Glucosidase;
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学科分类号
摘要
A new series of phthalimide-benzamide-1,2,3-triazole hybrids 8a–k as α-glucosidase inhibitors was designed and synthesized. The biological evaluation of compounds 8a–k against yeast α-glucosidase demonstrated that all they have excellent inhibitory activity in comparison with standard inhibitor acarbose. Among them, the most potent compound was compound 8d with inhibitory activity 18.5-fold more than acarbose. Kinetic study revealed that α-glucosidase inhibition of compound 8d was the competitive type. Furthermore, docking study suggested that compound 8d is more stable than acarbose in the active site of α-glucosidase.
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页码:868 / 876
页数:8
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