3-Hydroxy-N'-arylidenepropanehydrazonamides with Halo-Substituted Phenanthrene Scaffolds Cure P. berghei Infected Mice When Administered Perorally.

Michael Leven ; Tanja C Knaab ; Jana Held ; Sandra Duffy ; Stephan Meister ; Christoph Fischli ; Diane Meitzner ; Ursula Lehmann ; Beate Lungerich ; Krystina Kuna ; +8 more... Petra Stahlke ; Michael J Delves ORCID logo ; Mirko Buchholz ; Elizabeth A Winzeler ORCID logo ; Vicky M Avery ; Benjamin Mordmüller ; Sergio Wittlin ; Thomas Kurz ORCID logo ; (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. ISSN 0022-2623 DOI: 10.1021/acs.jmedchem.7b00140
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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.
Item Type Article
ISI 406727700006
Date Deposited 17 Aug 2018 16:03

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