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Design and synthesis of novel stiripentol analogues as potential anticonvulsants
Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt..
Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt..
Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt.;King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia..
Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Pharmacol Grp, Giza 12622, Egypt..ORCID iD: 0000-0002-5031-6391
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2012 (English)In: European Journal of Medicinal Chemistry, ISSN 0223-5234, E-ISSN 1768-3254, Vol. 47, 360-369 p.Article in journal (Refereed) PublishedText
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.

Place, publisher, year, edition, pages
2012. Vol. 47, 360-369 p.
Keyword [en]
Stiripentol, Epilepsy, Semicarbazones, Pyrazolines, Anticonvulsants
National Category
Biomedical Laboratory Science/Technology
Research subject
Biomedical Laboratory Science
Identifiers
URN: urn:nbn:se:kau:diva-41875DOI: 10.1016/j.ejmech.2011.11.004ISI: 000301169800039PubMedID: 22118828OAI: oai:DiVA.org:kau-41875DiVA: diva2:923059
Available from: 2016-04-25 Created: 2016-04-22 Last updated: 2016-07-08Bibliographically approved

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Maklad, Yousreya A.Abdel-Rehim, Mohamed
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