Synthesis and biological evaluation of new antiseizure compounds derived from valproic acid
Background: New hybrid compounds were synthesized by linking the valproic acid (VPA) structure with other anticonvulsant/anti-inflammatory scaffolds. Materials & methods: The chemistry involved the incorporation of the linker oxymethyl ester into VPA, followed by reaction with the second scaffold. The antiseizure effects were investigated by the maximal electroshock seizure test, and the most active compound was additionally evaluated in the 6 Hz test and pentylenetetrazol test in mice. Results: The compounds showed protection against seizures. The hybrid structure with the butylparaben scaffold exhibited an ED50 of 8.265 mg/kg (0.0236 mmol/Kg) in the maximal electroshock seizure test and 50.00 mg/kg (0.147 mmol/kg) in the 6 Hz test. Conclusion: The antiseizure activity of the synthesized compounds highlighted the potential of hybrid structures to treat multifactorial diseases such as epilepsy.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:15 |
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| Enthalten in: |
Future medicinal chemistry - 15(2023), 9 vom: 01. Mai, Seite 735-743 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Garofalo, Federico M [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 01.06.2023 Date Revised 02.06.2023 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2022-0222 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM357301145 |
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| 245 | 1 | 0 | |a Synthesis and biological evaluation of new antiseizure compounds derived from valproic acid |
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| 500 | |a Date Revised 02.06.2023 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Background: New hybrid compounds were synthesized by linking the valproic acid (VPA) structure with other anticonvulsant/anti-inflammatory scaffolds. Materials & methods: The chemistry involved the incorporation of the linker oxymethyl ester into VPA, followed by reaction with the second scaffold. The antiseizure effects were investigated by the maximal electroshock seizure test, and the most active compound was additionally evaluated in the 6 Hz test and pentylenetetrazol test in mice. Results: The compounds showed protection against seizures. The hybrid structure with the butylparaben scaffold exhibited an ED50 of 8.265 mg/kg (0.0236 mmol/Kg) in the maximal electroshock seizure test and 50.00 mg/kg (0.147 mmol/kg) in the 6 Hz test. Conclusion: The antiseizure activity of the synthesized compounds highlighted the potential of hybrid structures to treat multifactorial diseases such as epilepsy | ||
| 650 | 4 | |a Journal Article | |
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| 650 | 4 | |a codrugs | |
| 650 | 4 | |a epilepsy | |
| 650 | 4 | |a hybrid drugs | |
| 650 | 4 | |a multitarget drugs | |
| 650 | 4 | |a nipecotic acid | |
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| 700 | 1 | |a Sbaraglini, María L |e verfasserin |4 aut | |
| 700 | 1 | |a Barrionuevo, Emilia M |e verfasserin |4 aut | |
| 700 | 1 | |a Peralta, Estefanía |e verfasserin |4 aut | |
| 700 | 1 | |a Bonifazi, Evelyn L |e verfasserin |4 aut | |
| 700 | 1 | |a Talevi, Alan |e verfasserin |4 aut | |
| 700 | 1 | |a Gavernet, Luciana |e verfasserin |4 aut | |
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