Dapsone

Chemical Structure / Formula of Dapsone

  • Formula: C₁₂H₁₂N₂O₂S
  • Structure: Sulfonyl-containing diamine.

Dapsone

Mechanism of Action

  • Inhibits dihydropteroate synthase, similar to sulfonamides.

Uses

  • Leprosy (Mycobacterium leprae).
  • Pneumocystis pneumonia prophylaxis in HIV patients.

Side Effects

  • Hemolysis (especially in G6PD-deficient patients).
  • Methemoglobinemia, rash.

Synthesis of Dapsone

Synthesis of Dapsone

Structure-Activity Relationship (SAR) of Trimethoprim

Structural Feature SAR Insight
Diaminodiphenylsulfone core Mimics PABA and inhibits dihydropteroate synthase, similar to sulfonamides.
Aromatic amine groups Crucial for activity; acetylation leads to inactivation.
Sulfone linkage Important for antileprotic activity and stability.
Electron-donating groups May improve potency, while large substitutions decrease activity.

 

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