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).

A library of chiral tetrasubstituted diethylenetriamines was screened against Plasmodium falciparum. Compounds with MIC as low as 0.02 mg/mL were identified.Figure optionsDownload as PowerPoint slide