The Synthesis, Molecular Docking and CNS activity of 5, 5-diphenylimidazolidine-2, 4-dione derivatives

Synthesis of Phenytoin derivatives as CNS agents

Abstract

Abstract:

Background:  Epilepsy is a chronic non-communicable CNS disorder which affects large population of all ages. Different classes of drugs are used for the treatment of this neurological disorder but due to augmented drug resistance and side effects this drug become incompetent.     Therefore, we design the synthesis of ten new derivatives of Phenytoin. The moiety of Phenytoin was hybridized with different phenols by using three step approach. The synthesized molecules were then investigated for different physicochemical parameters such as Log P values using diverse software programs and to predict the potential to cross the blood brain barrier.

Objective: The new Phenytoin derivatives were synthesized, characterized, and compared for CNS activity with the previous synthesized compounds which contain anilines.

Method: Firstly, the chloroacetylation of the 5,5-diphenyl hydantoin was carried out and then various substituted phenols were added into it. The synthesized compounds were characterized and evaluated for antianxiety activity, muscle relaxant activity and anticonvulsant activity by using different models.

Result: The number of derivatives of 5,5-diphenyl hydantoin was developed and optimized. The number of parameters were optimized which reveal that the compound containing chloro group such as C3 and C6 showed imperative potential when compared with the standard drug Diazepam.

Conclusion: It was summarized that the new compounds of 5,5-diphenyl hydantoin derivatives were synthesized. The results of the data shows that the compound containing chloro group are more potent for CNS activity when compared to compound containing aniline group. The newly compounds have the probability to be optimized further to engender new scaffolds to treat various CNS disorders.

Keywords: Phenytoin, Parameters, CNS activity, blood brain barrier, Log P, CNS active.