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

Authors :
Mahmoud Biglar
Somayeh Mojtabavi
Abbas Rahmani
Mohammad Ali Faramarzi
Maryam Mohammadi-Khanaposhtani
Bagher Larijani
Seyed Esmaeil Sadat-Ebrahimi
Negar jafari
Azadeh Yahya-Meymandi
Mehdi Emadi
Mohammad Mahdavi
Source :
Medicinal Chemistry Research. 29:868-876
Publication Year :
2020
Publisher :
Springer Science and Business Media LLC, 2020.

Abstract

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.

Details

ISSN :
15548120 and 10542523
Volume :
29
Database :
OpenAIRE
Journal :
Medicinal Chemistry Research
Accession number :
edsair.doi...........c36455ba2f61ec9e0ddd6083002d3588