Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


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

Author(s): Anna M. Waszkielewicz, Edward Szneler, Marek Cegla, Henryk Marona.


A new series of N-(4-chlor-2-methylphenoxy)ethyl- (1-6) and N-(4-chlor-2-methylphenoxy)acetylaminoalkanols (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-1-ol, revealing 25% activity in MES at 30 mg/kg b.w. 0.5 and 1 h after administration.

Keywords: Alkanolamides, Aminoalkanols, Anticonvulsant, Epilepsy, Seizures, Synthesis, MES, Rotorod, neurotransmitter systems, lamotrigine

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Article Details

Year: 2013
Page: [35 - 43]
Pages: 9
DOI: 10.2174/1570180811309010035