Abstract

A series of 17 new aminoalkanol derivatives of 6-methoxy- or 7-chloro-2-methylxanthone as well as 6-methoxy-4-methylxanthone was synthesized and evaluated for anticonvulsant activity. All compounds were verified in mice after intraperitoneal (ip) administration in maximal electroshock (MES) and subcutaneous pentetrazole (scMet) induced seizures as well as neurotoxicity assessment. Eleven of the tested substances showed protection against electrically evoked seizures in the majority of the tested mice at the dose of 100mg/kg. Additionally, one was effective at the dose of 30mg/kg. Five substances were active at the dose of 300mg/kg or at the dose of 100mg/kg in the minority of the tested mice. The most promising compound revealed ED50 value of 47.57mg/kg in MES (mice, ip, 1h after administration) and at the same time its TD50 was evaluated as above 400mg/kg. Those values gave PI (calculated as TD50/ED50) of more than 8.41. Three other synthesized xanthone derivatives also proved to act as anticonvulsants and showed ED50 values in MES test (mice, ip) ranged 80–110mg/kg. Results were quite encouraging and suggested that in the group of xanthone derivatives new potential anticonvulsants might be found.

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