• Publications
  • Influence
The chemotherapy of rodent malaria. LX. The importance of formulation in evaluating the blood schizontocidal activity of some endoperoxide antimalarials
TLDR
The activities of artemisinin and a number of its semi-synthetic analogues, as well as Fenozan B07 (B07), a synthetic 1,2,4-trioxane, and arteflene (ATF) were compared in mice infected with drug-sensitive Plasmodium berghei or chloroquine-resistant P. yoelii ssp.
New developments in synthetic peroxidic drugs as artemisinin mimics.
The present review describes the current status of synthetic cyclic peroxides, trioxanes and trioxolanes that show significant promise as antimalarial drugs because of their artemisinin-like
Why artemisinin and certain synthetic peroxides are potent antimalarials. Implications for the mode of action.
  • C. W. Jefford
  • Chemistry, Medicine
    Current medicinal chemistry
  • 30 November 2001
TLDR
Experiments with ferrous reagents indicate that active peroxides including 14 and its congeners kill the parasite by alkylation with a sterically non-encumbered C-centered radical, however, another possibility is the involvement of a Fe(IV)=O species as the toxic agent.
The Deoxygenation and Isomerization of Artemisinin and Artemether and Their Relevance to Antimalarial Action
The treatment of artemisinin (1) and s-artemether (6) with Zn dissolving in AcOH for a few hours results in mono-deoxygenation giving deoxyartemisinin (5) and deoxy-s-artemether (7), respectively, as
Sulfur-containing polybromoindoles from the red alga Laurencia brongniartii
Abstract Six new polybromoindoles (9-14) have been isolated from the red alga Laurencia brongniartii. Two were optically active sulfoxides, the itomanindoles A (12) and B (13) and one was a bisindole
The Absolute Configurations and Biogenesis of Some New Halogenated Chamigrenes from the Sea Hare Aplysia dactylomela
Four new halogenated chamigrenes have been isolated from the sea hare, the (E)- and (Z)-9-(bromomethylidene)-1,2,5-trimethylspiro[5.5]undeca-1,7-dien-3-ones (11 and 10, resp.) the structures of which
The chemotherapy of rodent malaria. L. The activities of some synthetic 1,2,4-trioxanes against chloroquine-sensitive and chloroquine-resistant parasites. Part 3: Observations on 'Fenozan-50F', a
TLDR
The activity of Fenozan-50F is retained against a wide spectrum of drug-resistant parasite lines, although those highly resistant to quinine or to artemisinin are less responsive at the ED90 level.
Venustatriol. A new, anti-viral, triterpene tetracyclic ether from Laurencia venusta
Abstract Venustatriol, a new tetracyclic ether derived from squalene, which has anti-viral activity, has been isolated from the red alga Laurencia venusta . Its structure and absolute configuration
The chemotherapy of rodent malaria. XLIX. The activities of some synthetic 1,2,4-trioxanes against chloroquine-sensitive and chloroquine-resistant parasites. Part 2: Structure-activity studies on
TLDR
The activity of 51 synthetic cis-fused cyclopenteno-1,2,4-trioxanes has been examined against drug-sensitive and chloroquine-resistant malaria parasites in vivo and the most potent compound is Fenozan-50F.
...
1
2
3
4
5
...