Le Manach, ClairePaquet, TanyaBrunschwig, ChristelNjoroge, MathewHan, ZeCabrera, Diego GonzaalezBashyam, SrideviDhinakaran, RajkumarTaylor, DaleReader, JanetteBotha, M.E. (Mariette)Churchyard, AlisjeLauterbach, Sonja B.Coetzer, Theresa L.Birkholtz, Lyn-MarieMeister, StephanWinzeler, Elizabeth A.Waterson, DavidWitty, Michael J.Wittlin, SergioJimenez-Diaz, Maria-BelenMartinez, Maria SantosFerrer, SantiagoAngulo-Barturen, InigoStreet, Leslie J.Chibale, Kelly2016-02-292016-02-292015-10-26Le Manach, C, Paquet, T, Brunschwig, C, Njoroge, M, Han, Z, Gonzalez Cabrera, D, Bashyam, S, Dhinakaran, R, Taylor, D, Reader, J, Botha, M, Churchyard, A, Lauterbach, S, Coetzer, TL, Birkholtz, L-M, Meister, S, Winzeler, EA, Waterson, D, Witty, MJ, Wittlin, S, Jimenez-Diaz, M-B, Santos Martinez, M, Ferrer, S, Angulo-Barturen, I, Street, LJ & Chibale, K 2015, 'A novel pyrazolopyridine with in vivo activity in Plasmodium berghei- and Plasmodium falciparum-infected mouse models from structure-activity relationship studies around the core of recently identified antimalarial imidazopyridazines', Journal of Medicinal Chemistry, vol. 58, no. 21, pp. 8713-8722.0022-2623 (print)1520-4804 (online)10.1021/acs.jmedchem.5b01605http://hdl.handle.net/2263/51604Toward improving pharmacokinetics, in vivo efficacy, and selectivity over hERG, structure−activity relationship studies around the central core of antimalarial imidazopyridazines were conducted. This study led to the identification of potent pyrazolopyridines, which showed good in vivo efficacy and pharmacokinetics profiles. The lead compounds also proved to be very potent in the parasite liver and gametocyte stages, which makes them of high interest.en© 2015 American Chemical SocietyPharmacokineticsAntimalarial imidazopyridazinesPyrazolopyridinesParasite liverArticle