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Identification of fast-acting 2,6-disubstituted imidazopyridines that are efficacious in the In Vivo humanized Plasmodium falciparum nodscidil2rgamma (null) mouse model of malaria

Nchinda, Aloysius T. and Le Manach, Claire and Paquet, Tanya and Gonzàlez Cabrera, Diego and Wicht, Kathryn J. and Brunschwig, Christel and Njoroge, Mathew and Abay, Efrem and Taylor, Dale and Lawrence, Nina and Wittlin, Sergio and Jiménez-Díaz, María-Belén and Santos Martínez, María and Ferrer, Santiago and Angulo-Barturen, Iñigo and Lafuente-Monasterio, Maria Jose and Duffy, James and Burrows, Jeremy and Street, Leslie J. and Chibale, Kelly. (2018) Identification of fast-acting 2,6-disubstituted imidazopyridines that are efficacious in the In Vivo humanized Plasmodium falciparum nodscidil2rgamma (null) mouse model of malaria. Journal of medicinal chemistry, 61 (9). pp. 4213-4227.

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Official URL: https://edoc.unibas.ch/69265/

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Abstract

Optimization of a chemical series originating from whole-cell phenotypic screening against the human malaria parasite, Plasmodium falciparum, led to the identification of two promising 2,6-disubstituted imidazopyridine compounds, 43 and 74. These compounds exhibited potent activity against asexual blood stage parasites that, together with their in vitro absorption, distribution, metabolism, and excretion (ADME) properties, translated to in vivo efficacy with clearance of parasites in the PfSCID mouse model for malaria within 48 h of treatment.
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:05 Mar 2019 14:20
Deposited On:05 Mar 2019 14:20

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