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peroxides

Comparative embryotoxicity of different antimalarial peroxides: In vitro study using the rat whole embryo culture model (WEC)

November 26, 2010 - 13:05 -- Patrick Sampao
Author(s): 
Monica Longo, Sara Zanoncelli, Marco Brughera, Paolo Colombo, Sergio Wittlin, Jonathan L. Vennerstrom, Joerg Moehrle, J. Carl Craft
Reference: 
Reproductive Toxicology, Volume 30, Issue 4, December 2010, Pages 583-590

In an attempt to establish whether and to what extent activity as antimalarials and embryotoxicity can be divorced, IC50s for activity in Plasmodium falciparum strains and the NOELs for RBCs were compared. From this comparison, arterolane showed a better safety margin than artemisinin.

Technology: 

The comparative antimalarial properties of weak base and neutral synthetic ozonides

December 22, 2009 - 13:35 -- Patrick Sampao
Author(s): 
Yuanqing Tang, Sergio Wittlin, Susan A. Charman, Jacques Chollet, Francis C.K. Chiu, Julia Morizzi, Lisa M. Johnson, Josefina Santo Tomas, Christian Scheurer, Chistopher Snyder, Lin Zhou, Yuxiang Dong, William N. Charman, Hugues Matile, Heinrich Urwyler, Arnulf Dorn, Jonathan L. Vennerstrom
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 20, Issue 2, 15 January 2010, Pages 563-566

Thirty-three N-acyl 1,2,4-dispiro trioxolanes (secondary ozonides) were synthesized. For these ozonides, weak base functional groups were not required for high antimalarial potency against Plasmodium falciparum in vitro, but were necessary for high antimalarial efficacy in Plasmodium berghei-infected mice. A wide range of Log P/DpH 7.4 values were tolerated, although more lipophilic ozonides tended to be less metabolically stable.

Medical Treatment: 
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