The structure - activity relationship of the antimalarial ozonide arterolane (OZ277)

Yuxiang Dong, Sergio Wittlin, Kamaraj Sriraghavan, Jacques Chollet, Susan Ann Charman, William Neil Charman, Christian Scheurer, Heinrich Urwyler, Josefina Santo Tomas, Christopher Snyder, Darren John Creek, Julia Morizzi, Maria Koltun, Hugues Matile, Xiaofang Wang, Maniyan Padmanilayam, Yuanqing Tang, Arnulf Dorn, Reto Brun, Jonathan Vennerstrom

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Abstract

The structure and stereochemistry of the cyclohexane substituents of analogues of arterolane (OZ277) had little effect on potency against Plasmodium falciparum in vitro. Weak base functional groups were not required for high antimalarial potency, but they were essential for high antimalarial efficacy in P. berghei-infected mice. Five new ozonides with antimalarial efficacy and ADME profiles superior or equal to that of arterolane were identified.
Original languageEnglish
Pages (from-to)481 - 491
Number of pages11
JournalJournal of Medicinal Chemistry
Volume53
DOIs
Publication statusPublished - 2010

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