The Structure−Activity Relationship of the Antimalarial Ozonide Arterolane (OZ277)
Yuxiang Dong(Nebraska Medical Center), Sergio Wittlin(Swiss Tropical and Public Health Institute), K. Sriraghavan(University of Nebraska Medical Center), Jacques Chollet(Swiss Tropical and Public Health Institute), Susan A. Charman(Monash University), William N. Charman(Monash University), Christian Scheurer(Swiss Tropical and Public Health Institute), Heinrich Urwyler(Basilea Pharmaceutica (Switzerland)), Josefina Santo Tomas(Monash University), Christopher M. Snyder(Swiss Tropical and Public Health Institute), Darren J. Creek(Monash University), Julia Morizzi(Monash University), Maria Koltun(Monash University), Hugues Matile(Roche (Switzerland)), Xiaofang Wang(University of Nebraska Medical Center), Maniyan P. Padmanilayam(University of Nebraska Medical Center), Yuanqing Tang(Nebraska Medical Center), Arnulf Dorn(Roche (Switzerland)), Reto Brun(Swiss Tropical and Public Health Institute), Jonathan L. Vennerstrom(University of Nebraska Medical Center)
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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.
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