| Literature DB >> 1501229 |
J L Vennerstrom1, H N Fu, W Y Ellis, A L Ager, J K Wood, S L Andersen, L Gerena, W K Milhous.
Abstract
Dispiro-1,2,4,5-tetraoxanes 2-4 were synthesized as potential peroxide antimalarial drugs. They had curative activity against Plasmodium berghei in vivo at single doses of 320 and 640 mg/kg which confirms earlier unpublished data. Moreover, artemisinin (1) and 4 had equivalent ED50's against P. berghei in vivo in the multiple-dose Thompson test; neither showed any evidence of acute toxicity at total doses of more than 12 g/kg. Dispiro-1,2,4,5-tetraoxane 4 had IC50's comparable to those of 1 against Plasmodium falciparum clones in vitro. These results confirm the potential of dispiro-1,2,4,5-tetraoxanes as a new class of inexpensive peroxide antimalarial drugs.Entities:
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Year: 1992 PMID： 1501229 DOI： 10.1021/jm00094a015
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446