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Design and synthesi...
Design and synthesis of novel stiripentol analogues as potential anticonvulsants
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- Aboul-Enein, Mohamed N. (author)
- Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt.
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- El-Azzouny, Aida A. (author)
- Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt.
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- Attia, Mohamed I. (author)
- 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.
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- Maklad, Yousreya A. (author)
- Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Pharmacol Grp, Giza 12622, Egypt.
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- Amin, Kamilia M. (author)
- Cairo Univ, Fac Pharm, Dept Pharmaceut Chem, Cairo, Egypt.
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- Abdel-Rehim, Mohamed (author)
- Karlstads universitet,Avdelningen för kemi och biomedicinsk vetenskap
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- El-Behairy, Mohammed F. (author)
- Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Med Chem Grp, Giza 12622, Egypt.
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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. (creator_code:org_t)
- Elsevier BV, 2012
- 2012
- English.
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In: European Journal of Medicinal Chemistry. - : Elsevier BV. - 0223-5234 .- 1768-3254. ; 47, s. 360-369
- Related links:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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- 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.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinsk bioteknologi -- Biomedicinsk laboratorievetenskap/teknologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Medical Biotechnology -- Biomedical Laboratory Science/Technology (hsv//eng)
Keyword
- Stiripentol
- Epilepsy
- Semicarbazones
- Pyrazolines
- Anticonvulsants
- Biomedical Laboratory Science
- Biomedicinsk laboratorievetenskap
Publication and Content Type
- ref (subject category)
- art (subject category)
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