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