The Structure−Activity Relationship of the Antimalarial Ozonide Arterolane (OZ277)
Journal of Medicinal Chemistry2009Vol. 53(1), pp. 481–491
Citations Over TimeTop 10% of 2009 papers
Yuxiang Dong, Sergio Wittlin, K. Sriraghavan, Jacques Chollet, Susan A. Charman, William N. Charman, Christian Scheurer, Heinrich Urwyler, Josefina Santo Tomas, Christopher M. Snyder, Darren J. Creek, Julia Morizzi, Maria Koltun, Hugues Matile, Xiaofang Wang, Maniyan P. Padmanilayam, Yuanqing Tang, Arnulf Dorn, Reto Brun, Jonathan L. Vennerstrom
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.
Related Papers
- → oxygenated chalcones and bischalcones as potential antimalarial agents(2000)126 cited
- → Antimalarial Activity of Kaempferol and Its Combination with Chloroquine in Plasmodium berghei Infection in Mice(2018)45 cited
- → Study of the antimalarial properties of hydroxyethylamine derivatives using green fluorescent protein transformed Plasmodium berghei(2015)9 cited
- → Evaluation of the Ex vivo Antimalarial Activity of Organotin (IV) Ethylphenyldithiocarbamate on Erythrocytes Infected With Plasmodium berghei Nk 65(2014)6 cited
- Studies on 2,3,N,N'-substituted 4,4'-diaminodiphenylsulfones as potential antimalarial agents.(1989)