Antimalarial and cytotoxic activities of chiral triamines

Chiral triamine antimalarial compounds have been identified following the screening of mixture-based positional scanning libraries made up of 31,320 compounds against P. falciparum. The library, namely N-methyl triamine (TPI 762) was generated following exhaustive reduction of resin-bound acylated dipeptides. Using the PSCL approach, individual compounds were rapidly identified which were only 10 times less active than the standard drugs chloroquine (CQ) and Artemisinin (Artes).

Graphical abstractA library of chiral tetrasubstituted diethylenetriamines was screened against Plasmodium falciparum. Compounds with MIC as low as 0.02 mg/mL were identified.Figure optionsDownload full-size imageDownload as PowerPoint slide