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The comparative antimalarial properties of weak base and neutral synthetic ozonides

December 22, 2009 - 13:35 -- Patrick Sampao
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
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.

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Open Access | Pharmaceutical and Medicinal Chemistry: Falcipain-2 inhibitors

December 17, 2009 - 13:34 -- Kabogo Ndegwa
Roberta Ettari, Floriana Bova, Maria Zappalà, Silvana Grasso, Nicola Micale
Medicinal Research Reviews, Volume 30 Issue 1, Pages 136 – 167

This review is focused on inhibitors of falcipain-2, a cysteine protease from P. falciparum, which represents one of the most promising targets for antimalarial drug design.


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