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- W4328048266 abstract "Aim: α-Glucosidase inhibitors are important oral antidiabetic drugs that are used alone or in combination therapy. Materials & methods: In this regard, 1,3,4-thiadiazoles–1,2,3-triazoles were designed, synthesized and evaluated for α-glucosidase enzyme inhibition. Results: The applied synthesis protocol involved a ‘click’ reaction between a novel alkyne derived from a 1,3,4-thiadiazole derivative and phenylacetamide azides. The hybrid (9n) bearing 2-methyl and 4-nitro substituents was the best inhibitor with an IC 50 value of 31.91 μM (acarbose IC 50 = 844.81 μM). The blind molecular docking study of the best derivative (9n) showed that it interacted with the allosteric site's amino acid residues of α-glucosidase. Conclusion: 'Click'-inspired potential α-glucosidase inhibitors (1,3,4-thiadiazole–1,2,3-triazole hybrids) were identified and structure–activity relationship and kinetic and molecular docking studies accomplished." @default.
- W4328048266 created "2023-03-22" @default.
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- W4328048266 date "2023-02-01" @default.
- W4328048266 modified "2023-10-16" @default.
- W4328048266 title "Inhibition of α-glucosidase enzyme by ‘click'-inspired pharmacophore framework 1,3,4-thiadiazole–1,2,3-triazole hybrids" @default.
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- W4328048266 doi "https://doi.org/10.4155/fmc-2022-0289" @default.
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