Screening of the Tres Cantos Anti-Malarial Set, a database of two-million structures made available by pharmaceutical giant GlaxoSmithKline (GSK), London, UK, has led to the identification of a series of cyclopropyl carboxamides through rapid “triaging” of three series of related compounds.
One of these compounds (pictured) has been shown to have potent in vitro activity against the malaria parasite Plasmodium falciparum. It also has good oral bioavailability and shows a promising dose-activity relationship in a mouse model of malaria. The new series of antimalarials emerges from a collaboration between Medicines for Malaria Venture, Geneva, Switzerland, and GSK scientists.
- Cyclopropyl Carboxamides: A New Oral Antimalarial Series Derived from the Tres Cantos Anti-Malarial Set (TCAMS)
L. Rueda, I. Castellote, J. Castro-Pichel, M. J. Chaparro, J. C. de la Rosa et al.,
ACS Med. Chem. Lett. 2011.