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April 1, 2026Scientific AfricanOpen Access

Synthesis, Alpha glycosidase Activities and Molecular Docking study of Novel 4-amino-2H-1,2,4-triazol-3(4H)-one Schiff base derivatives

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Authors

EYEmmanuel Oloruntoba YeyeDADolapo L. AshiruEOEjike Onwudiegwu Okpala

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Overview

Novel Schiff base derivatives exhibit significant α-glucosidase inhibition in antidiabetic research, indicating potential therapeutic benefits.

Key Points

  • The aim is to synthesize and evaluate the inhibitory activity of 4-amino-2H-1,2,4-triazol-3(4H)-one Schiff base derivatives.
  • Synthesis via modified Boulton-Katritzky method
  • Characterization using 1H-NMR and EI-MS
  • Evaluation of α-glucosidase inhibition
  • Molecular docking studies
  • ADMET profiling
  • Compounds 2, 3, 4, 5, and 10 showed IC₅₀ values of 12.4 ± 0.43 to 17.5 ± 0.36 µM
  • Compound 6 exhibited the best inhibition with an IC₅₀ of 11.4 ± 0.56 µM, outperforming acarbose
  • Structure-activity relationship revealed enhancements with polyhydroxylation and methoxy substitution
  • Molecular docking indicated strong affinities for compounds 4 and 5, comparable to known inhibitors
  • Most compounds met Lipinski’s and Pfizer’s rules for drug-likeness

Cite This Study

Yeye et al. (2026) studied this question.

synapsesocial.com/papers/69ccb59f16edfba7beb876bahttps://doi.org/10.1016/j.sciaf.2026.e03338
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