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
Letters in Drug Design & Discovery
Title:Synthesis and Evaluation of Anticonvulsant Activity of Some N-[(4-Chlor- 2-methylphenoxy)ethyl]- and N-[(4-Chlor-2-methylphenoxy)acetyl]aminoalkanols
Volume: 10 Issue: 1
Author(s): Anna M. Waszkielewicz, Edward Szneler, Marek Cegla and Henryk Marona
Affiliation:
Keywords: Alkanolamides, Aminoalkanols, Anticonvulsant, Epilepsy, Seizures, Synthesis, MES, Rotorod, neurotransmitter systems, lamotrigine
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.
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M. Waszkielewicz Anna, Szneler Edward, Cegla Marek and Marona Henryk, Synthesis and Evaluation of Anticonvulsant Activity of Some N-[(4-Chlor- 2-methylphenoxy)ethyl]- and N-[(4-Chlor-2-methylphenoxy)acetyl]aminoalkanols, Letters in Drug Design & Discovery 2013; 10 (1) . https://dx.doi.org/10.2174/1570180811309010035
DOI https://dx.doi.org/10.2174/1570180811309010035 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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