Sulfonamides · Pharmacology

Which structural feature is essential for the antimicrobial activity of a sulfonamide molecule?

  1. A free amino group para to the sulfonamide group
  2. A long hydrocarbon chain on the sulfur atom
  3. Substitution of the sulfur atom with a phosphorus atom
  4. A nitro group attached to the benzene ring
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Correct answer: A free amino group para to the sulfonamide group

Antimicrobial activity requires a free amino group in the para-position relative to the sulfonamide group. Substitution on this para-amino group abolishes activity unless the substituent is removed in vivo, as happens with prodrugs such as sulfasalazine.

Difficulty: Medium Question 18 of 20

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