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.
Highlights
Malaria is still one of the most severe infectious diseases
The progress of the reaction was monitored by TLC
After 2–9 h the reaction mixture was extracted with a saturated sodium hydrogen carbonate solution, with a hydrogen chloride solution (10%), with brine and with water
Summary
Malaria is still one of the most severe infectious diseases. 3.2 billion people are at risk of being infected. Despite a decreasing number of mortal cases in the last decade due to better vector control and artemisinine-based combination therapy (ACT), still 584,000 deaths caused by malaria infection were reported in 2013 [1]. There are effective chemotherapeutics for the treatment of malaria, the discovery of new drugs is important due to the increasing resistances against available drugs [2,3]. A good strategy to circumvent the problem of resistance is to develop compounds acting with new mechanisms of action. There is an urgent need for compounds with novel chemotypes which differ from scaffolds of existing drugs
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