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

摘要: 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. TCAMS provides variety of starting points investigation new antiplasmodial drug leads. One promising compounds TCMDC-137332, seemed to be good point due its potency and predicted physicochemical properties. Several analogues based on 2-phenoxyanilide scaffold were synthesized by standard amide coupling reactions fully characterized regarding their identity purity spectroscopic chromatographic methods. Furthermore, results biological evaluation all congeners falciparum NF54 strains are presented. findings our in vitro screening could not confirm presumed nanomolar TCMDC-137332 derivatives.