Aza-Michael approach for the rapid synthesis of 3,5-dimethylpyrazole derivatives with potential biological significance.

A promising strategy for preventing epileptogenic processes involves the development of modified aza-Michael adducts, which demonstrate a range of biological activities, including antioxidant, anti-inflammatory, and antiviral effects. In the present study, compound 3, administered at a dose of 50 mg/kg, prevented pentylenetetrazole-induced clonic seizures in 60% of mice (ED50 = 37.5 mg/kg), while compound 4 achieved seizure prevention in 40% of mice. With an ED50 value of 155.5 mg/kg, compound 3 was approximately four times more potent than ethosuximide. Importantly, neither the tested compounds nor ethosuximide (50-500 mg/kg) produced muscle relaxation or impaired motor coordination. Furthermore, derivatives of compound 3 exhibited not only anticonvulsant activity but also anxiolytic and antidepressant effects, surpassing ethosuximide in the conducted assays. Ongoing research aims to further explore and optimize this series of compounds for potential therapeutic use.