Synthesis, physicochemical and anticonvulsant properties of some amino
isopropanoloxy 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 fo
r neurotoxicity in the rotorod test in mice and rats. The most promisi
ng compounds seem to be the 3-(tert.-butyl-amino) (3), 3-[N-methyl-(te
rt.-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.