VENNERSTROM, JONATHAN L.,DONG, YUXIANG,CHARMAN, SUSAN A.,WITTLIN, SERGIO,CHOLLET, JACQUES,CREEK, DARREN J.,WANG, XIAOFANG,SRIRAGHAVAN, KAMARAJ,ZHOU, LIN,MATILE, HUGUES,CHARMAN, WILLIAM N.
申请号:
PL08845311
公开号:
PL2203457T3
申请日:
2008.10.29
申请国别(地区):
PL
年份:
2014
代理人:
摘要:
A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites. The compounds of the invention unexpectedly provide a single-dose cure for malaria, as well as prophylactic activity against the same. The compounds are also active against schistosomiasis and cancer.