25 research outputs found
Kondensierte Ringsysteme des Oxadiazols, 2. Mitt. [1]: Synthese von neuen 2-Aryl-1,3,4-oxadiazolo[3,2-a]-s-triazin-5,7(6H)-dionen
Kondensierte Ringsysteme des Benzimidazols, 6. Mitt.: Organische Azide in der Heterocyclen-Synthese, 10. Mitt.: Synthese von substituierten Pyrimido[1,6-a]benzimidazolen als m�gliche antimikrobielle Wirkstoffe
Kondensierte Thiazole, 1. Mitt.: Synthese von 5,7-disubstituierten Thiazolo[4,5-d]pyrimidinen als potentielle anti-HIV, anticancerogene und antimikrobielle Verbindungen
Kondensiere Thiazole, 2. Mitt.: Synthese. von 7-substituierten Thiazolo[4,5-d]pyrimidinen als potentielle anti-HIV, anticancerogene und antimikrobielle Verbindungen
Discovery and structure-activity relationships of pyrrolone antimalarials
In the pursuit of new antimalarial leads, a phenotypic screening of various commercially sourced compound libraries was undertaken by the World Health Organisation Programme for Research and Training in Tropical Diseases (WHO-TDR). We report here the detailed characterization of one of the hits from this process, TDR32750 (8a), which showed potent activity against Plasmodium falciparum K1 (EC50 approximately 9 nM), good selectivity (<2000-fold) compared to a mammalian cell line (L6), and significant activity against a rodent model of malaria when administered intraperitoneally. Structure-activity relationship studies have indicated ways in which the molecule could be optimized. This compound represents an exciting start point for a drug discovery program for the development of a novel antimalaria