SYNTHESIS AND EVALUATION OF ANTICONVULSANT ACTIVITY OF N-(2,5-DIMETHYLPHENOXY)- AND N-[(2,3,5-TRIMETHYLPHENOXY)ALKYL]AMINOALKANOLS

摘要

A series of new N-(2,5-dimethylphenoxy)-and N-(2,3,5-trimethylphenoxy)alkylaminoalkanols [I XVII] was synthesized and evaluated for anticonvulsant activity. Pharmacological tests included maximal electroshock (IVIES) and subcutaneous pentetrazole seizure threshold (scMet) assays as well as neurotoxicity (TOX) evaluation in mice after intraperitoneal (i.p.) administration and/or in rats after oral (p.o.) administration. The most active compound was R-2N-[(2,3,5-trimethylphenoxy)ethyl]aminobutan-1-ol, which exhibited 100% activity in MES at the dose of 30 mg/kg body weight (mice, i.p.) and 75% activity in MES at 30 mg/kg b.w. (rats, p.o.) without neurotoxicity at the active doses.