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
JournalArticle (Originalarbeit in einer wissenschaftlichen Zeitschrift)
 
ID 3395654
Author(s) 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, Iñigo; Street, Leslie J.; Chibale, Kelly
Author(s) at UniBasel Wittlin, Sergio
Year 2015
Title 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 Journal of medicinal chemistry
Volume 58
Number 21
Pages / Article-Number 8713-8722
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.
Publisher American Chemical Society
ISSN/ISBN 0022-2623
edoc-URL http://edoc.unibas.ch/41499/
Full Text on edoc No
Digital Object Identifier DOI 10.1021/acs.jmedchem.5b01605
PubMed ID http://www.ncbi.nlm.nih.gov/pubmed/26502160
ISI-Number WOS:000364796100028
Document type (ISI) Article
 
   

MCSS v5.8 PRO. 0.425 sec, queries - 0.000 sec ©Universität Basel  |  Impressum   |    
07/08/2020