期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 3, 页码 864-868出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.11.051
关键词
1,3,4-Oxadiazoles; Semicarbazones; Limonene; Citral; Anticonvulsant activity
资金
- AICTE New Delhi, India
Two novel series of N-4-(5-(2/3/4-substituted-phenyl)-1,3,4-oxadiazol-2-yl)-N-1-(2-methyl-5-(prop-1-en-2-yl)cyclohex-2-enylidene)semicarbazide and N-4-(5-(2/3/4-substituted-phenyl)-1,3,4-oxadiazol-2-yl)-N-1-(3,7-dimethylocta-3,6-dienylidene)-semicarbazide were synthesized to meet structural prerequisite indispensable for anticonvulsant activity. The anticonvulsant activities of the compounds were investigated using maximal electroshock seizure (MES), subcutaneous pentylenetrtrazole (scPTZ) and subcutaneous strychnine (scSTY) models. The rotorod test was conducted to evaluate neurotoxicity. Some of the selected active compounds were subjected to GABA assay to confirm their mode of action. The outcome of the present investigations proved that the four binding sites pharmacophore model is vital for anticonvulsant activity. The efforts were also made to establish structure-activity relationships among test compounds. (c) 2012 Elsevier Ltd. All rights reserved.
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