Medicinal Chemistry: Anticonvulsants, Antipsychotics & SAR
Anticonvulsant Drugs
Anticonvulsants are agents used to prevent or control seizures by reducing abnormal, excessive neuronal activity in the brain.
Classification
- Hydantoins: Phenytoin
- Succinimides: Ethosuximide
- Iminostilbenes: Carbamazepine
- Barbiturates: Phenobarbital
- Others: Valproic acid, Diazepam
General SAR
- Hydrophobic aromatic ring is essential.
- Electron-withdrawing groups increase activity by improving membrane penetration.
- Imide or amide groups are critical for binding.
- Optimal lipophilicity is required; excessive polarity leads to inactivity, while excessive lipophilicity causes toxicity.
- Planarity increases CNS activity by facilitating receptor binding.
General Mechanism of Action
Anticonvulsants act by blocking Na⁺ channels, enhancing GABA activity,... Continue reading "Medicinal Chemistry: Anticonvulsants, Antipsychotics & SAR" »
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