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

Dong, Y. and Wittlin, S. and Sriraghavan, K. and Chollet, J. and Charman, S. A. and Charman, W. N. and Scheurer, C. and Urwyler, H. and Santo, T. J. and Snyder, C. and Creek, D. J. and Morizzi, J. and Koltun, M. and Matile, H. and Wang, X. and Padmanilayam, M. and Tang, Y. and Dorn, A. and Brun, R. and Vennerstrom, J. L.. (2010) The structure-activity relationship of the antimalarial ozonide arterolane (OZ277). Journal of Medicinal Chemistry, 53 (1). pp. 481-491.

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Official URL: http://edoc.unibas.ch/dok/A5843050

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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
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Brun, Reto and Wittlin, Sergio
Item Type:Article, refereed
Bibsysno:Link to catalogue
Publisher:American Chemical Society
ISSN:0022-2623
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:19 Oct 2017 07:07
Deposited On:08 Jun 2012 06:47

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