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  • Title: Aminoalkanolic derivatives of xanthone with potential antiepileptic activity.
    Author: Marona H, Górka Z, Szneler E.
    Journal: Pharmazie; 1998 Apr; 53(4):219-23. PubMed ID: 9583083.
    Abstract:
    Synthesis, physicochemical and anticonvulsant properties of some aminoisopropanoloxy derivatives of 2-xanthone are described. The compounds were prepared by the amination of 2-[(2,3-epoxy)-propoxyl]-xanthone or 2-(3-chloro-2-hydroxy-propoxy)-xanthone. The obtained compounds were evaluated for anticonvulsant activity in the maximal electroshock (MES)- and subcutaneous pentylenetetrazole (scMet)-induced seizures and for neurotoxicity in the rotorod test in mice and rats. The most promising compounds seem to be the 3-(tert.-butyl-amino) (3), 3-[N-methyl-(tert.-butyl)-amino] (12) and 3-[4-(benzyl)-1-piperazinyl (5) substituted 2-hydroxy-1-(2-xanthonoxy)-propane from which 3 and 5 were active in both the anticonvulsant tests. The protective index (TD50/ED50) in MES in mice for 3 and valproate, as for 12 and phenytoin or carbamazepine, is similar.
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