Question:
What will happen if the electron-withdrawing group at position-7 is substituted in benzodiazepines
What will happen if the electron-withdrawing group at position-7 is substituted in benzodiazepines
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Pos-7 EWG = High potency. Think "7 is Heaven" for benzodiazepine activity.
Updated On: May 25, 2026
- Reduce GABA - A receptor binding
- Increase Anxiolytic Activity
- Reduce Protein binding
- Solubility will increase
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The Correct Option is B
Solution and Explanation
Step 1: Concept
The Structure-Activity Relationship (SAR) of benzodiazepines dictates how specific substitutions alter their sedative and anxiolytic properties.
Step 2: Meaning
Position-7 of the benzodiazepine ring is a critical site for determining the potency of the molecule.
Step 3: Analysis
An electronegative (electron-withdrawing) substituent, such as a halogen (e.g., Chlorine in Diazepam) or a nitro group (e.g., in Nitrazepam), at position-7 is essential for high anxiolytic activity.
Step 4: Conclusion
Therefore, placing or increasing the strength of an electron-withdrawing group at this position increases the drug's activity. Final Answer: (B)
The Structure-Activity Relationship (SAR) of benzodiazepines dictates how specific substitutions alter their sedative and anxiolytic properties.
Step 2: Meaning
Position-7 of the benzodiazepine ring is a critical site for determining the potency of the molecule.
Step 3: Analysis
An electronegative (electron-withdrawing) substituent, such as a halogen (e.g., Chlorine in Diazepam) or a nitro group (e.g., in Nitrazepam), at position-7 is essential for high anxiolytic activity.
Step 4: Conclusion
Therefore, placing or increasing the strength of an electron-withdrawing group at this position increases the drug's activity. Final Answer: (B)
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