Aloysius T Nchinda, Claire Le Manach, Tanya Paquet, Diego Gonzalez Cabrera, Kathryn J Wicht, Christel Brunschwig, Mathew Njoroge, Efrem Abay, Dale Taylor, Nina Lawrence, Sergio Wittlin, Maria-Belen Jimenez-Diaz, Maria Santos Martínez-Martínez, Santiago Ferrer, Iñigo Angulo-Barturen, Maria Jose Lafuente-Monasterio, James Duffy, Jeremy N Burrows, Leslie J Street, Kelly Chibale
Optimization of a chemical series originating from whole-cell phenotypic screening against the human malaria parasite, Plasmodium falciparum, led to the identification of two promising 2,6-disubstituted imidazopyridine compounds, 43 and 74. These compounds exhibited potent activity against asexual blood stage parasites that, together with their in vitro Absorption, Distribution, Metabolism, and Excretion (ADME) properties, translated to in vivo efficacy with clearance of parasites in the PfSCID mouse model for malaria within 48 h of treatment...
April 17, 2018: Journal of Medicinal Chemistry