SYNTHESIS AND ANTICONVULSANT EFFECTS OF SOME AMINOALKANOLIC DERIVATIVES OF XANTHONE

Synthesis and physicochemical properties of alkanolamine derivatives o f xanthone are described. Alkanolamines were synthesized by of the rea ction of an appropriate aminoalcohol with corresponding 2-bromomethylx anthones. The obtained compounds 1-13 were evaluated for anticonvulsan t activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure threshold (scMet) assays and for neurotoxic ity (TOX). Several alkanolamines were found to be active in both the a nticonvulsant 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 i ndex (TD50/ED50) in the range 2.21-5.84 corresponding with that for ph enytoin, carbamazepine and valproate.