The Structure−Activity Relationship of the Antimalarial Ozonide Arterolane (OZ277)

Autor:	Jonathan L. Vennerstrom, Heinrich Urwyler, Sergio Wittlin, Yuxiang Dong, Darren J. Creek, Yuanqing Tang, Arnulf Dorn, Kamaraj Sriraghavan, Christopher Snyder, Julia Morizzi, Reto Brun, Maniyan Padmanilayam, Maria Koltun, Susan A. Charman, William N. Charman, Jacques Chollet, Xiaofang Wang, Hugues Matile, Josefina Santo Tomas, Christian Scheurer
Rok vydání:	2009
Předmět:	Stereochemistry Plasmodium falciparum Molecular Conformation Antimalarials Heterocyclic Compounds 1-Ring Mice Structure-Activity Relationship chemistry.chemical_compound Parasitic Sensitivity Tests parasitic diseases Drug Discovery Animals Structure–activity relationship Ozonide Potency Spiro Compounds Malaria Falciparum Arterolane ADME biology Chemistry Stereoisomerism biology.organism_classification Peroxides Molecular Medicine
Zdroj:	Journal of Medicinal Chemistry. 53:481-491
ISSN:	1520-4804 0022-2623
DOI:	10.1021/jm901473s
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::597e9be51453d7021377a69512c5262a https://doi.org/10.1021/jm901473s Zobrazit plný text záznamu