Tetraoxanes as antimalarials: harnessing the endoperoxide.
With the emergence of resistance to artemesinin, the need for new antimalarial compounds is pressing. Several research groups have made significant contributions to the exploration of the use of 1,2,4,5-tetraoxanes and 1,2,4- trioxanes as synthetic analogues of artemesinin. This short review highlights the recent developments in this field detailing both biological results and useful synthetic methodology. In addition, the current understanding of the mode of action of this class of compounds has been described.
Laura C
LC
Fisher
Stellenbosch University, Department of Chemistry and Polymer Science, Private Bag X1, Matieland, 7602, Stellenbosch, South Africa. mblackie@sun.ac.za.
Margaret A L
MA
Blackie
D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D008288:Malaria / Q000188:drug therapy*; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D010545:Peroxides / Q000737:chemistry*; D010963:Plasmodium falciparum / Q000187:drug effects*; D010966:Plasmodium vivax / Q000187:drug effects*; D013329:Structure-Activity Relationship; D045568:Tetraoxanes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
D000962:Antimalarials; D010545:Peroxides; D045568:Tetraoxanes