Antimalarial and cytotoxic activities of chiral triamines.
Afef Dellai;
Jon Appel;
Abderrahman Bouraoui;
Simon Croft ;
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
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).
Item Type | Article |
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Keywords | Chiral amines, Antimalrial, Malaria, Solid-phase organic synthesis, Libraries, Mixtures based libraries, Parallel synthesis, combinatorial chemistry, derivatives, libraries, diversity, trends |
ISI | 322611900017 |
ORCID: https://orcid.org/0000-0002-3902-8006