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3-hydroxy-N'-arylidenepropanehydrazonamides with halo-substituted phenanthrene scaffolds cure P. berghei infected mice when administered perorally

Leven, Michael and Knaab, Tanja C. and Held, Jana and Duffy, Sandra and Meister, Stephan and Fischli, Christoph and Meitzner, Diane and Lehmann, Ursula and Lungerich, Beate and Kuna, Krystina and Stahlke, Petra and Delves, Michael J. and Buchholz, Mirko and Winzeler, Elizabeth A. and Avery, Vicky M. and Mordmüller, Benjamin and Wittlin, Sergio and Kurz, Thomas. (2017) 3-hydroxy-N'-arylidenepropanehydrazonamides with halo-substituted phenanthrene scaffolds cure P. berghei infected mice when administered perorally. Journal of Medicinal Chemistry, 60 (14). pp. 6036-6044.

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Official URL: http://edoc.unibas.ch/55876/

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Abstract

Structural optimization of 3-hydroxy-N'-arylidenepropanehydrazonamides provided new analogs with nanomolar to subnanomolar antiplasmodial activity against asexual blood stages of Plasmodium falciparum, excellent parasite selectivity, and nanomolar activity against the earliest forms of gametocyte development. Particularly, derivatives with a 1,3-dihalo-6-trifluoromethylphenanthrene moiety showed outstanding in vivo properties and demonstrated in part curative activity in the Plasmodium berghei mouse model when administered perorally.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
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 and Lehmann, Ursula
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:American Chemical Society
ISSN:0022-2623
e-ISSN:1520-4804
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:20 Oct 2017 06:48
Deposited On:20 Oct 2017 06:29

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