Anticonvulsant and neurotoxicity evaluation of some novel kojic acids and allomaltol derivatives

Archiv der Pharmazie
Mutlu Dilsiz Aytemir, Unsal Calis

Abstract

A series of new 3-hydroxy-6-hydroxymethyl/methyl-2-substituted 4H-pyran-4-ones were synthesized and prepared by the reaction of kojic acid or allomaltol with piperidine derivatives and formaline as potential anticonvulsant compounds. The structure of the synthesized compounds was confirmed using the elemental analysis results and the spectroscopic techniques such as IR, 1H-NMR, and ESI-MS. Anticonvulsant activities were examined by maximal electroshock (MES) and subcutaneous Metrazol (scMet)-induced seizure tests. Neurotoxicity was determined by the rotorod toxicity test. All these tests were performed in accordance with the procedures of the Antiepileptic Drug Development (ADD) program. According to the activity studies and at all doses, 3-hydroxy-2-[(4-hydroxy-4-phenylpiperidin-1-yl)methyl]-6-methyl-4H-pyran-4-one (compound 1), 2-{[4-(4-chlorophenyl)-3,6-dihydropyridin-1(2H)-yl]methyl}-3-hydroxy-6-methyl-4H-pyran-4-one (compound 6), 2-[(4-acetyl-4-phenylpiperidin-1-yl)methyl]-3-hydroxy-6-(hydroxymethyl)-4H-pyran-4-one (compound 11), and 2-{[4-(4-chlorophenyl)-3,6-dihydropyridin-1(2H)-yl] methyl}-3-hydroxy-6-hydroxymethyl-4H-pyran-4-one (compound 12) were found to have anticonvulsant activity against MES-induced seizures at 4 ...Continue Reading

References

Aug 1, 1978·Epilepsia·R L KrallE A Swinyard
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Nov 26, 2002·European Journal of Medicinal Chemistry·Gülcan OztürkTayfun Uzbay
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Sep 18, 2007·European Journal of Medicinal Chemistry·Lotfollah S DehkordiRobert C Hider

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Citations

Dec 3, 2014·European Journal of Medicinal Chemistry·Gheorghe Roman
Apr 4, 2012·Journal of Enzyme Inhibition and Medicinal Chemistry·Gülşah KarakayaÜnsal Calış
May 24, 2021·European Journal of Medicinal Chemistry·Min HeGuangcheng Wang

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