Antimalarial and cytotoxic activities of chiral triamines.

Afef Dellai; Jon Appel; Abderrahman Bouraoui; Simon Croft ORCID logo; Adel Nefzi; (2013) Antimalarial and cytotoxic activities of chiral triamines. Bioorganic & medicinal chemistry letters, 23 (16). pp. 4579-4582. ISSN 0960-894X DOI: 10.1016/j.bmcl.2013.06.035
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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).

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