SAR of Oxazolidinediones

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Chapter: Medicinal Chemistry : Anticonvulsants

Replacement of the -NH group at position 1 of the hydantoin system with an oxygen atom yields the oxazolidine-2,4-dione system.


SAR of Oxazolidinediones


  • Replacement of the -NH group at position 1 of the hydantoin system with an oxygen atom yields the oxazolidine-2,4-dione system.

  • 3,5,5-Trimethadione (tridione) was the first drug introduced specifically for treating absence seizures. It is also important as a prototype structure.

  • The nature of the substituent on C-5 is important, example, lower alkyl substituents towards antipetitmal activity while acyl substituents towards antigrandmal activity.

  • The N-alkyl substituent does not alter or afford the activity since all the clinically used agents from this class undergo N-dealkylation in metabolism.

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