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Novel piperazine-linked sulfonamide derivatives were synthesized and evaluated as inhibitors of glutathione S-transferase pi 1 (GSTP1-1). These compounds exhibit significant inhibitory potential, with promising drug-likeness and ADMET profiles for therapeutic development.

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Area of Science:

  • Medicinal Chemistry
  • Enzyme Inhibition
  • Drug Discovery

Background:

  • Glutathione S-transferase pi 1 (GSTP1-1) is a key enzyme implicated in various diseases, making it a significant therapeutic target.
  • Developing novel inhibitors for GSTP1-1 is crucial for advancing treatment strategies.
  • Existing inhibitors may have limitations, necessitating the exploration of new chemical scaffolds.

Purpose of the Study:

  • To synthesize and characterize novel sulfonamide derivatives containing the piperazine moiety.
  • To evaluate the inhibitory activity of these synthesized compounds against GSTP1-1.
  • To investigate the binding interactions and drug-likeness of the potential inhibitors.

Main Methods:

  • Synthesis of sulfonamide derivatives via the Povarov reaction.
  • Structural characterization using NMR, IR, and mass spectroscopy.
  • Enzyme inhibition assays, Lineweaver-Burk analysis, molecular docking, molecular dynamics, and in silico ADMET predictions.

Main Results:

  • Synthesized piperazine-linked sulfonamide derivatives (PLSDs) demonstrated significant GSTP1-1 inhibition with IC50 values ranging from 0.33 to 0.86 µM.
  • Calculated inhibition constants (Ki) ranged from 1.443 ± 0.562 to 4.192 ± 0.125 µM.
  • Molecular docking and dynamics revealed strong binding interactions with the GSTP1-1 active site, and in silico analysis indicated favorable drug-likeness and ADMET properties.

Conclusions:

  • The novel PLSDs are potent inhibitors of GSTP1-1.
  • These compounds possess favorable pharmacokinetic properties, suggesting their potential as therapeutic agents.
  • The study provides valuable structural insights for the rational design of next-generation GSTP1-1 inhibitors for targeted therapies.