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Aboul-Enein, M. N., El-Azzouny, A. A., Attia, M. I., Maklad, Y. A., Amin, K. M., Abdel-Rehim, M. & El-Behairy, M. F. (2012). Design and synthesis of novel stiripentol analogues as potential anticonvulsants. European Journal of Medicinal Chemistry, 47, 360-369
Open this publication in new window or tab >>Design and synthesis of novel stiripentol analogues as potential anticonvulsants
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2012 (English)In: European Journal of Medicinal Chemistry, ISSN 0223-5234, E-ISSN 1768-3254, Vol. 47, p. 360-369Article in journal (Refereed) Published
Abstract [en]

A series of stiripentol (SIP) analogues namely, 2-1(1E)-1-(1,3-benzodioxol-5-yl)-4,4-dimethylpent-1-en-3-ylidene]-N-(aryl/H)hydrazinecarboxamides 7a-h, (+/-)-(5RS)-N-(aryl/H)-(1,3-benzodioxol-5-yl)-3-tert-butyl-4,5-dihydro-1H-pyrazole-1-carboxamides (+/-)-8a-h, and (+/-)-[(5RS)-(1,3-benzodioxol-5-yl)-3-tert-butyl-4,5-dihydro-1H-pyrazol-1-yl](aryl)methanones (+/-)-13a-f was synthesized by adopting appropriate synthetic routes and was pharmacologically evaluated in the preliminary anticonvulsant screens. The selected bioactive new chemical entities were subjected to ED50 determination and neurotoxicity evaluation. The most active congeners are 7h in MES screen and (+/-)-13b in scPTZ screen which displayed ED50 values of 87 and 110 mg/kg, respectively, as compared to that of STP (ED50 = 277.7 and 115 mg/kg in MES and scPTZ, respectively). (C) 2011 Elsevier Masson SAS. All rights reserved.

Keywords
Stiripentol, Epilepsy, Semicarbazones, Pyrazolines, Anticonvulsants
National Category
Biomedical Laboratory Science/Technology
Research subject
Biomedical Laboratory Science
Identifiers
urn:nbn:se:kau:diva-41875 (URN)10.1016/j.ejmech.2011.11.004 (DOI)000301169800039 ()22118828 (PubMedID)
Available from: 2016-04-25 Created: 2016-04-22 Last updated: 2019-12-09Bibliographically approved
Identifiers
ORCID iD: ORCID iD iconorcid.org/0000-0002-5031-6391

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