| Literature DB >> 26502160 |
Claire Le Manach, Tanya Paquet, Christel Brunschwig1, Mathew Njoroge1, Ze Han, Diego Gonzàlez Cabrera, Sridevi Bashyam2, Rajkumar Dhinakaran2, Dale Taylor1, Janette Reader3, Mariette Botha3, Alisje Churchyard3, Sonja Lauterbach3, Theresa L Coetzer4, Lyn-Marie Birkholtz3, Stephan Meister5, Elizabeth A Winzeler5, David Waterson6, Michael J Witty6, Sergio Wittlin7,8, María-Belén Jiménez-Díaz9, María Santos Martínez9, Santiago Ferrer9, Iñigo Angulo-Barturen9, Leslie J Street, Kelly Chibale.
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.Entities:
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Year: 2015 PMID: 26502160 DOI: 10.1021/acs.jmedchem.5b01605
Source DB: PubMed Journal: J Med Chem ISSN: 0022-2623 Impact factor: 7.446