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Structure-Activity Relationship (SAR) of Anticonvulsants

The structure-activity relationship (SAR) of anticonvulsants is quite complex due to the diverse nature of these drugs. However, some general trends can be observed:

  1. Many anticonvulsants have a basic center (often an amine) which is important for their activity.

  2. In general, lipophilicity is important for anticonvulsant activity, as these drugs need to cross the blood-brain barrier to reach their site of action.

  3. For many anticonvulsants, a balance between lipophilicity and water solubility is necessary for optimal activity. Too much lipophilicity can lead to poor water solubility, which can limit the absorption of the drug.

  4. In many anticonvulsants, the presence of aromatic rings can enhance activity. For example, phenytoin contains a phenyl ring, and carbamazepine contains a biphenyl structure.


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