Synthesis and Evaluation of Anticonvulsant Activity of Some N-[(4-Chlor-2-methylphenoxy)ethyl]- and N-[(4-Chlor-2-methylphenoxy)acetyl]amino-alkanols

摘要

A new series of iV-(4-chlor-2-methylphenoxy)ethyl- (1-6) and iV-(4-chlor-2-methylphenoxy)acetyl-aminoalkanols (7-10) has been synthesized for evaluation of their anticonvulsant activity. Pharmacological tests included maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure (ScMet) assays, as well as rotarod for neurotoxicity (TOX) and were performed in mice i.p. and rats p.o. The activity of the compounds in the group was various, and the most active compound in mice was R,S-1N-[(4-chlor-2-methylphenoxy)ethyl]aminopropan-2-ol, revealing 100% activity in MES test at 30 mg/kg b.w., 0.5 h after administration without toxicity at the same dose and time. In rats (p.o), the most active compound was 2N-[(4-chlor-2-methylphenoxy)ethyl]amino-2-methylpropan-l-ol, revealing 25% activity in MES at 30 mg/kg b.w. 0.5 and 1 h after administration.