Question:

Which statement best describes the mechanism of action of azole antifungals?

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They block 14-alpha-demethylase in the ergosterol pathway.
Updated On: Jun 23, 2026
  • Inhibition of synthesis of ergosterol
  • Inhibition of thymidylate synthase
  • Targeting beta-1,3-glucan
  • Disruption of cell wall
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The Correct Option is A

Solution and Explanation

Step 1: Ergosterol is the principal sterol of the fungal cell membrane and is essential for membrane fluidity and integrity. Step 2: Azole antifungals (fluconazole, itraconazole, ketoconazole and others) act by inhibiting 14-alpha-lanosterol demethylase, a cytochrome P450 enzyme that is a key step in ergosterol biosynthesis. Step 3: This blockade depletes ergosterol and causes accumulation of toxic 14-alpha-methylated sterols in the fungal membrane, which disrupts membrane function and destroys the fungus. Step 4: Thymidylate synthase inhibition relates to flucytosine, targeting beta-1,3-glucan is the action of echinocandins, and direct cell wall disruption is not the azole mechanism. Hence inhibition of ergosterol synthesis is correct.
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