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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

Le Manach, Claire and Paquet, Tanya and Brunschwig, Christel and Njoroge, Mathew and Han, Ze and Gonzàlez Cabrera, Diego and Bashyam, Sridevi and Dhinakaran, Rajkumar and Taylor, Dale and Reader, Janette and Botha, Mariette and Churchyard, Alisje and Lauterbach, Sonja and Coetzer, Theresa L. and Birkholtz, Lyn-Marie and Meister, Stephan and Winzeler, Elizabeth A. and Waterson, David and Witty, Michael J. and Wittlin, Sergio and Jiménez-Díaz, María-Belén and Santos Martínez, María and Ferrer, Santiago and Angulo-Barturen, Iñigo and Street, Leslie J. and Chibale, Kelly. (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, 58 (21). pp. 8713-8722.

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Official URL: http://edoc.unibas.ch/41499/

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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.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Wittlin, Sergio
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:American Chemical Society
ISSN:0022-2623
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:20 Oct 2017 06:22
Deposited On:13 Apr 2016 11:58

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