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<p>A new series of [1,2,4]triazolo[1,5-<i>a</i>]pyrimidine-7(4<i>H</i>)-one derivatives was designed, synthesized, and evaluated as potent anticonvulsant agents in pentylenetetrazole (PTZ) and maximal electroshock (MES) induced seizure models in mice. Latency times to the first symptom of seizure were measured, and the recorded data demonstrated that most of the newly synthesized compounds exhibited anticonvulsant activity in the PTZ test. Among them, the 4-bromobenzyl derivative showed the best anticonvulsant activity and was also the most potent compound in the MES assay. Considering that the new scaffold possesses the necessary pharmacophore units to act as a benzodiazepine receptor (BZDR) agonist, this most potent derivative was further evaluated in vivo and in silico for BZDR agonist activity. The in vivo evaluation using flumazenil, a BZDR antagonist, confirmed agonist action of the most potent compound at the BZDR.</p> Graphical Abstract <p></p>

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Design, synthesis, in vivo, and in silico studies of new [1,2,4] triazolo[1,5-a]pyrimidine-7(4H)-one derivatives as potent anticonvulsant agents

  • 期刊论文

  • 发表日期：

    2026年6月28日

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  • Mehregan Fallah-Kolamsary,
  • Hassan Kabirifard,
  • Ahmad Reza Dehpour,
  • Mohammad Mahdavi,
  • Maryam Mohammadi-Khanaposhtani

摘要

A new series of [1,2,4]triazolo[1,5-a]pyrimidine-7(4H)-one derivatives was designed, synthesized, and evaluated as potent anticonvulsant agents in pentylenetetrazole (PTZ) and maximal electroshock (MES) induced seizure models in mice. Latency times to the first symptom of seizure were measured, and the recorded data demonstrated that most of the newly synthesized compounds exhibited anticonvulsant activity in the PTZ test. Among them, the 4-bromobenzyl derivative showed the best anticonvulsant activity and was also the most potent compound in the MES assay. Considering that the new scaffold possesses the necessary pharmacophore units to act as a benzodiazepine receptor (BZDR) agonist, this most potent derivative was further evaluated in vivo and in silico for BZDR agonist activity. The in vivo evaluation using flumazenil, a BZDR antagonist, confirmed agonist action of the most potent compound at the BZDR.

Graphical Abstract