Journal of Medicinal Chemistry p. 8713 - 8722 (2015)
Update date:2022-08-05
Topics:
Le Manach, Claire
Paquet, Tanya
Brunschwig, Christel
Njoroge, Mathew
Han, Ze
Gonzàlez Cabrera, Diego
Bashyam, Sridevi
Dhinakaran, Rajkumar
Taylor, Dale
Reader, Janette
Botha, Mariette
Churchyard, Alisje
Lauterbach, Sonja
Coetzer, Theresa L.
Birkholtz, Lyn-Marie
Meister, Stephan
Winzeler, Elizabeth A.
Waterson, David
Witty, Michael J.
Wittlin, Sergio
Jiménez-Díaz, María-Belén
Santos Martínez, María
Ferrer, Santiago
Angulo-Barturen, I?igo
Street, Leslie J.
Chibale, Kelly
Toward 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.
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