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The comparative antimalarial properties of weak base and neutral synthetic ozonides

Submitted by patrick sampao on December 22, 2009 - 13:35
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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
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Contact email: 
jvenners@unmc.edu

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.

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