A 4-butyl-2,7-bis(2-fluorophenyl)-triazolopyrimidin-5(4H)-one compound, and a preparation method and use thereof

By designing and synthesizing a novel 4-butyl-2,7-bis(2-fluorophenyl)-triazolopyrimidine-5(4H)-one compound, the sedation and motor incoordination side effects of existing antiepileptic drugs were solved, achieving a highly effective antiepileptic treatment without significant neurotoxicity.

CN119899191BActive Publication Date: 2025-11-18QINGDAO UNIV OF SCI & TECH +1
4 Cites 0 Cited by

Patent Information

Application Number
CN202411959295.5
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2024-12-30
Publication Date
2025-11-18
Estimated Expiration
2044-12-30

AI Technical Summary

Technical Problem

Existing [1,2,4]-triazolo[1,5-a]pyrimidine-7-one heterocyclic compounds have side effects such as sedation and motor incoordination when used to treat epilepsy, making it difficult to meet the demand for antiepileptic drugs with low neurotoxicity.

Method used

A novel 4-butyl-2,7-bis(2-fluorophenyl)-triazolopyrimidine-5(4H)-one compound was developed. Through specific structural design and synthetic methods, the compound was ensured to have antiepileptic activity with almost no sedative or motor incoordination side effects.

Benefits of technology

The compound exhibited significant antiepileptic activity in mouse models, with an ED50 value of 9.17 mg/kg and a TD50 value of >813.40 mg/kg. Its anticonvulsant activity was superior to that of the positive control drug, and it showed no neurotoxicity at saturated solubility, indicating promising clinical application prospects.

✦ Generated by Eureka AI based on patent content.
Patent Text Reader

Abstract

The application discloses a 4-butyl-2,7-bis(2-fluorophenyl)-triazolopyrimidine-5(4H)-ketone compound and a preparation method and application thereof. The anti-convulsion activity of the compound is evaluated by adopting a subcutaneous pentylenetetrazol (Sc-PTZ) and a mouse maximum electroshock (MES) model, and the neurotoxicity of the compound is evaluated by adopting a rotating rod method; experimental data show that the target compound with the structure of formula I provided by the application has clear and strong anti-convulsion activity and extremely low neurotoxicity, and the conclusion proves that the compound with the structure of formula I has the possibility of being developed into a new type of epilepsy treatment drug with low neurotoxicity.
Need to check novelty before this filing date? Find Prior Art