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New phthalimide-benzamide-1,2,3-triazole hybrids; design, synthesis, α-glucosidase inhibition assay, and docking study
- 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.
- Subjects :
- 1,2,3-Triazole
biology
010405 organic chemistry
Stereochemistry
Organic Chemistry
Active site
01 natural sciences
Yeast
0104 chemical sciences
Phthalimide
010404 medicinal & biomolecular chemistry
chemistry.chemical_compound
chemistry
Design synthesis
Docking (molecular)
biology.protein
medicine
General Pharmacology, Toxicology and Pharmaceutics
Benzamide
Acarbose
medicine.drug
Subjects
Details
- ISSN :
- 15548120 and 10542523
- Volume :
- 29
- Database :
- OpenAIRE
- Journal :
- Medicinal Chemistry Research
- Accession number :
- edsair.doi...........c36455ba2f61ec9e0ddd6083002d3588