The Antimalarial Set

  • Author: David Bradley
  • Published: 12 September 2011
  • Copyright: Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
  • Source / Publisher: ACS Medicinal Chemistry Letters/ACS Publications
thumbnail image: The Antimalarial Set

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.

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