Synthesis and anticonvulsant effects of some aminoalkanolic derivatives of xanthone.

Synthesis and physicochemical properties of alkanolamine derivatives of xanthone are described. Alkanolamines were synthesized by of the reaction of an appropriate aminoalcohol with corresponding 2-bromomethylxanthones. The obtained compounds 1-13 were evaluated for anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure threshold (scMet) assays and for neurotoxicity (TOX). Several alkanolamines were found to be active in both the anticonvulsant tests. Most interesting were the 2-amino-1-propanol-, 1-amino-2-propanol- or 1-amino-2-butanol derivatives of 6-methoxy- or 6-chloroxanthone, which displayed anti MES activity with a protective index (TD50/ED50) in the range 2.21-5.84 corresponding with that for phenytoin, carbamazepine and valproate.