Design, synthesis and anticonvulsant-analgesic activity of new N-[(phenoxy)alkyl]- and N-[(phenoxy)ethoxyethyl]aminoalkanols

The takeaway

Aminoalkanol derivatives displayed promising anticonvulsant and analgesic effects in mice, with no toxicity in cell-based tests, suggesting they could be strong candidates for antiepileptic drug development

The science

Dozens of synthetic derivatives were tested in seizure models, including the maximum electroshock and pentylenetetrazol-induced convulsions. Several compounds showed high protection against seizures, with effects similar to standard reference drugs. Some also reduced pain responses in the formalin test, indicating dual benefits as anticonvulsants and pain relievers. Notably, they did not cause motor impairment in the rotarod or chimney tests, and most had no sedative effects. In vitro assays confirmed the safety of these compounds for liver and glial cells, with no signs of toxicity. One compound, a piperidin-3-ol derivative, stood out as the most promising, offering strong seizure protection along with favorable safety and pharmacokinetic predictions.

Why it matters

By combining seizure protection and pain relief with low toxicity, these compounds could become templates for safer, multifunctional therapies to manage epilepsy.

Original article

https://doi.org/10.1039/c6md00537c