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The comparative antimalarial properties of weak base and neutral synthetic ozonides

Tang, Y. and Wittlin, S. and Charman, S. A. and Chollet, J. and Chiu, F. C. and Morizzi, J. and Johnson, L. M. and Tomas, J. S. and Scheurer, C. and Snyder, C. and Zhou, L. and Dong, Y. and Charman, W. N. and Matile, H. and Urwyler, H. and Dorn, A. and Vennerstrom, J. L.. (2010) The comparative antimalarial properties of weak base and neutral synthetic ozonides. Bioorganic and Medicinal Chemistry Letters, Vol. 20, H. 2. pp. 563-566.

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Official URL: http://edoc.unibas.ch/dok/A5843042

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Abstract

Thirty-three N-acyl 1,2,4-dispiro trioxolanes (secondary ozonides) were synthesized. For these ozonides, weak base functional groups were not required for high antimalarial potency against Plasmodium falciparum in vitro, but were necessary for high antimalarial efficacy in Plasmodium berghei-infected mice. A wide range of LogP/D(pH)(7.4) values were tolerated, although more lipophilic ozonides tended to be less metabolically stable
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Wittlin, Sergio
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Pergamon
ISSN:0960-894X
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:08 Jun 2012 06:55
Deposited On:08 Jun 2012 06:46

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