Pyridine sulfonamide as a small key organic molecule for the potential treatment of type-II diabetes mellitus and Alzheimer’s disease: In vitro studies against yeast α-glucosidase, acetylcholinesterase and butyrylcholinesterase

Oct 10, 2015Bioorganic chemistry

Pyridine sulfonamide as a small molecule that may help treat type 2 diabetes and Alzheimer's by blocking key enzymes in lab tests

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Abstract

Compound 4a demonstrated significant inhibition against α-glucosidase (IC50 32.2±0.3μM), acetylcholinesterase (IC50 50.2±0.8μM), and butyrylcholinesterase (IC50 43.8±0.8μM).

  • The synthesis of novel pyridine 2,4,6-tricarbohydrazide derivatives yielded high activity against α-glucosidase and cholinesterases.
  • Most compounds showed stronger inhibition of yeast α-glucosidase compared to the reference compound acarbose (IC50 38.25±0.12μM).
  • Compound 4c, featuring a 4-fluoro benzyl group, was identified as the most potent inhibitor of α-glucosidase with an IC50 of 25.6±0.2μM.
  • Compound 4a exhibited significant inhibition across all three tested enzymes.
  • Molecular modeling studies were conducted on compound 4a to explore its interaction patterns with α-glucosidase and acetylcholinesterase.

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