Studies on New Schiff bases of Benzoxazole: Synthesis, Anticonvulsant and Neurotoxicity Evaluation

Abstract

Twelve Schiff bases of benzoxazole were prepared by usage of methyl-3-amino-4hydroxybenzoate. The chemistry of the prepared molecules was established based on the spectral data and tested for anticonvulsant activity using maximal electroshock (MES) induced seizure and subcutaneous pentylenetetrazole (scPTZ). In addition, a rotarod method to detect minimal neurological impairment in mice. In anti-MES test molecules 3d, 3e, 3i, 3j and 3k presented effective action corresponding to hydrophobicity. Other compounds of the series like 3b, 3c, 3g and 3l were remarkably less lipophilic and have some potencies. Compounds 3d and 3j effectively passed the rotarod trial without any mark of CNS deficit. In conclusion, the synthesized compounds with distal aryl groups showed higher hydrophobicity and resulted in better pharmacological action, which can be the future of new promising anticonvulsant drugs.