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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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 and Henryk Marona

Volume 10, Issue 1, 2013

Page: [35 - 43] Pages: 9

DOI: 10.2174/1570180811309010035

Price: $65

Abstract

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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