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Molecules 2016, 21(2), 223; doi:10.3390/molecules21020223

Novel 2-Phenoxyanilide Congeners Derived from a Hit Structure of the TCAMS: Synthesis and Evaluation of Their in Vitro Activity against Plasmodium falciparum

1
Institut für Medizinische und Pharmazeutische Chemie, Technische Universität Braunschweig, Beethovenstraße 55, 38106 Braunschweig, Germany
2
Department of Microbiology and Molecular Genetics, IMRIC, The Kuvin Center for the Study of Infectious and Tropical Diseases, The Hebrew University-Hadassah Medical School, Jerusalem 91120, Israel
3
Center of Pharmaceutical Engineering (PVZ), Technische Universität Braunschweig, Franz-Liszt-Straße 35A, 38106 Braunschweig, Germany
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 18 December 2015 / Revised: 29 January 2016 / Accepted: 2 February 2016 / Published: 17 February 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [1813 KB, uploaded 17 February 2016]   |  

Abstract

The Tres Cantos Antimalarial Compound Set (TCAMS) is a publicly available compound library which contains 13533 hit structures with confirmed activity against Plasmodium falciparum, the infective agent responsible for malaria tropica. The TCAMS provides a variety of starting points for the investigation of new antiplasmodial drug leads. One of the promising compounds is TCMDC-137332, which seemed to be a good starting point due to its antiplasmodial potency and its predicted physicochemical properties. Several new analogues based on a 2-phenoxyanilide scaffold were synthesized by standard amide coupling reactions and were fully characterized regarding their identity and purity by spectroscopic and chromatographic methods. Furthermore, the results of the biological evaluation of all congeners against Plasmodium falciparum NF54 strains are presented. The findings of our in vitro screening could not confirm the presumed nanomolar antiplasmodial activity of TCMDC-137332 and its derivatives. View Full-Text
Keywords: diarylether; luciferase; Malaria; 2-phenoxyanilide; Plasmodium falciparum; TCAMS; TCMDC-137332 diarylether; luciferase; Malaria; 2-phenoxyanilide; Plasmodium falciparum; TCAMS; TCMDC-137332
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Weidner, T.; Nasereddin, A.; Preu, L.; Grünefeld, J.; Dzikowski, R.; Kunick, C. Novel 2-Phenoxyanilide Congeners Derived from a Hit Structure of the TCAMS: Synthesis and Evaluation of Their in Vitro Activity against Plasmodium falciparum. Molecules 2016, 21, 223.

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