Mefenamic Acid

• Mefenamic Acid is an NSAID effective in treating pain, inflammation, and menstrual cramps.
• It inhibits COX enzymes, reducing prostaglandin synthesis for analgesic and anti-inflammatory action.

Chemical Formula:

• C₁₅H₁₅NO₂

Mechanism:

• Reversible, non-selective COX inhibitor
• Reduces prostaglandin synthesis → pain relief, anti-inflammatory

Uses:

• Dysmenorrhea
• Mild to moderate pain
• Musculoskeletal inflammation

Side Effects:

• GI irritation
• Diarrhea
• CNS effects (dizziness, drowsiness)
• Renal impairment (rare)

SAR of Mefenamic Acids:

1. Anthranilic acid core (fenamate):

   • Key structure shared with other fenamates.

2. Two aryl rings:

   • One attached directly to nitrogen (aniline-type), the other on benzoic acid core → necessary for COX inhibition.

3. Ortho-position carboxylic acid:

   • Interacts with the active site of COX enzyme (anchors the molecule).

4. Aromatic substitution:

   • Electron-donating groups can enhance potency.

5. Planar structure:

   • Facilitates insertion into COX binding site.

Synthesis of Mefenamic Acid:

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