Publication: 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, A.T Le Manach, C Paquet, T Gonzalez Cabrera, D Wicht, K.J Brunschwig, C Njoroge, M Abay, E Taylor, D Lawrence, N
Nchinda, A.T
Le Manach, C
Paquet, T
Gonzalez Cabrera, D
Wicht, K.J
Brunschwig, C
Njoroge, M
Abay, E
Taylor, D
Lawrence, N
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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.
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Date
2018-04-17
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Publisher
ACS Publications
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Research Projects
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Keywords
Malaria,Parasites,Plasmodium falciparum
Citation
Aloysius T. Nchinda, Claire Le Manach, Tanya Paquet, Diego Gonzà lez Cabrera, Kathryn J. Wicht, Christel Brunschwig, Mathew Njoroge, Efrem Abay, Dale Taylor, Nina Lawrence, Sergio Wittlin, MarÃa-Belén Jiménez-DÃaz, MarÃa Santos MartÃnez, Santiago Ferrer, Iñigo Angulo-Barturen, Maria Jose Lafuente-Monasterio, James Duffy, Jeremy Burrows, Leslie J. Street, and Kelly Chibale Journal of Medicinal Chemistry 2018 61 (9), 4213-4227 DOI: 10.1021/acs.jmedchem.8b00382