Question

According to the SAR of Chloroquine, electron:

• A. Withdrawing group at 6th position of the quinoline ring is important for the inhibition of hemozoin formation
• B. Donating group at 7th position of the quinoline ring is important for the inhibition of hemozoin formation
• C. Donating group at 6th position of the quinoline ring is important for the inhibition of hemozoin formation
• D. Withdrawing group at 7th position of the quinoline ring is important for the inhibition of hemozoin formation

Hint:

- Chloroquine’s antimalarial activity depends on its ability to inhibit hemozoin formation. - Electron-withdrawing groups at the 7th position enhance this inhibition. - Electron-donating groups decrease efficacy by altering drug-target interactions.

Answer 1

The Correct Option is D

The Structure-Activity Relationship (SAR) of Chloroquine indicates that the quinoline ring plays a crucial role in the drug's ability to inhibit hemozoin formation, which is essential for its antimalarial activity. The presence of an electron-withdrawing group at the 7th position of the quinoline ring enhances the drug’s potency by stabilizing interactions with the target site and inhibiting the polymerization of heme into hemozoin.