Design and synthesis of novel stiripentol analogues as potential anticonvulsants
2012 (English)In: European Journal of Medicinal Chemistry, ISSN 0223-5234, E-ISSN 1768-3254, Vol. 47, 360-369 p.Article in journal (Refereed) Published
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.
Stiripentol, Epilepsy, Semicarbazones, Pyrazolines, Anticonvulsants
Biomedical Laboratory Science/Technology
Research subject Biomedical Laboratory Science
IdentifiersURN: urn:nbn:se:kau:diva-41875DOI: 10.1016/j.ejmech.2011.11.004ISI: 000301169800039PubMedID: 22118828OAI: oai:DiVA.org:kau-41875DiVA: diva2:923059