TY - JOUR
T1 - The structure - activity relationship of the antimalarial ozonide arterolane (OZ277)
AU - Dong, Yuxiang
AU - Wittlin, Sergio
AU - Sriraghavan, Kamaraj
AU - Chollet, Jacques
AU - Charman, Susan Ann
AU - Charman, William Neil
AU - Scheurer, Christian
AU - Urwyler, Heinrich
AU - Santo Tomas, Josefina
AU - Snyder, Christopher
AU - Creek, Darren John
AU - Morizzi, Julia
AU - Koltun, Maria
AU - Matile, Hugues
AU - Wang, Xiaofang
AU - Padmanilayam, Maniyan
AU - Tang, Yuanqing
AU - Dorn, Arnulf
AU - Brun, Reto
AU - Vennerstrom, Jonathan
PY - 2010
Y1 - 2010
N2 - 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.
AB - 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.
U2 - 10.1021/jm901473S
DO - 10.1021/jm901473S
M3 - Article
VL - 53
SP - 481
EP - 491
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
ER -