ANTIMALARIALLY POTENT, EASILY PREPARED, FLUORINATED ENDOPEROXIDES

Three or four step chemical synthesis and in vitro antimalarial testin g showed crystalline, thermally stable, bicyclic endoperoxides 3c and 4c to be potent antimalarials, having approximately 15% of the antimal arial activity of the clinically used, complex, sesquiterpene, lactone , natural product artemisinin (qinghaosu, 1). A novel mechanism involv ing reactive alkylating agents is proposed to account for the ability of endoperoxides 3c and 4c to kill malaria parasites. Copyright (C) 19 96 Elsevier Science Ltd