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
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Date
Authors
Le Manach, Claire
Paquet, Tanya
Brunschwig, Christel
Njoroge, Mathew
Han, Ze
Cabrera, Diego Gonzaalez
Bashyam, Sridevi
Dhinakaran, Rajkumar
Taylor, Dale
Reader, Janette
Journal Title
Journal ISSN
Volume Title
Publisher
American Chemical Society
Abstract
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.
Description
Keywords
Pharmacokinetics, Antimalarial imidazopyridazines, Pyrazolopyridines, Parasite liver
Sustainable Development Goals
Citation
Le 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.