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

Yuxiang Dong, Sergio Wittlin, Kamaraj Sriraghavan, Jacques Chollet, Susan A. Charman, William N. Charman, Christian Scheurer, Heinrich Urwyler, Josefina Santo Tomas, Christopher Snyder, Darren J. Creek, Julia Morizzi, Maria Koltun, Hugues Matile, Xiaofang Wang, Maniyan Padmanilayam, Yuanqing Tang, Arnulf Dorn, Reto Brun, Jonathan L. 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 (US)
Pages (from-to)481-491
Number of pages11
JournalJournal of Medicinal Chemistry
Volume53
Issue number1
DOIs
StatePublished - Jan 28 2010

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ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this

Dong, Y., Wittlin, S., Sriraghavan, K., Chollet, J., Charman, S. A., Charman, W. N., Scheurer, C., Urwyler, H., Tomas, J. S., Snyder, C., Creek, D. J., Morizzi, J., Koltun, M., Matile, H., Wang, X., Padmanilayam, M., Tang, Y., Dorn, A., Brun, R., & Vennerstrom, J. L. (2010). The structure - Activity relationship of the antimalarial ozonide arterolane (OZ277). Journal of Medicinal Chemistry, 53(1), 481-491. https://doi.org/10.1021/jm901473s