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Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγ null Mouse Model of Malaria.
Nchinda, Aloysius T; Le Manach, Claire; Paquet, Tanya; Gonzàlez Cabrera, Diego; Wicht, Kathryn J; Brunschwig, Christel; Njoroge, Mathew; Abay, Efrem; Taylor, Dale; Lawrence, Nina; Wittlin, Sergio; Jiménez-Díaz, María-Belén; Santos Martínez, María; Ferrer, Santiago; Angulo-Barturen, Iñigo; Lafuente-Monasterio, Maria Jose; Duffy, James; Burrows, Jeremy; Street, Leslie J; Chibale, Kelly.
Afiliación
  • Nchinda AT; Drug Discovery and Development Center (H3D), Department of Chemistry , University of Cape Town , Rondebosch 7701 , South Africa.
  • Le Manach C; Drug Discovery and Development Center (H3D), Department of Chemistry , University of Cape Town , Rondebosch 7701 , South Africa.
  • Paquet T; Drug Discovery and Development Center (H3D), Department of Chemistry , University of Cape Town , Rondebosch 7701 , South Africa.
  • Gonzàlez Cabrera D; Drug Discovery and Development Center (H3D), Department of Chemistry , University of Cape Town , Rondebosch 7701 , South Africa.
  • Wicht KJ; Drug Discovery and Development Center (H3D), Department of Chemistry , University of Cape Town , Rondebosch 7701 , South Africa.
  • Brunschwig C; Drug Discovery and Development Center (H3D), Division of Clinical Pharmacology, Department of Medicine , University of Cape Town , Observatory, Cape Town 7925 , South Africa.
  • Njoroge M; Drug Discovery and Development Center (H3D), Division of Clinical Pharmacology, Department of Medicine , University of Cape Town , Observatory, Cape Town 7925 , South Africa.
  • Abay E; Drug Discovery and Development Center (H3D), Division of Clinical Pharmacology, Department of Medicine , University of Cape Town , Observatory, Cape Town 7925 , South Africa.
  • Taylor D; Drug Discovery and Development Center (H3D), Division of Clinical Pharmacology, Department of Medicine , University of Cape Town , Observatory, Cape Town 7925 , South Africa.
  • Lawrence N; Drug Discovery and Development Center (H3D), Division of Clinical Pharmacology, Department of Medicine , University of Cape Town , Observatory, Cape Town 7925 , South Africa.
  • Wittlin S; Swiss Tropical and Public Health Institute , Socinstrasse 57 , 4002 Basel , Switzerland.
  • Jiménez-Díaz MB; University of Basel , 4003 Basel , Switzerland.
  • Santos Martínez M; GlaxoSmithKline, Tres Cantos Medicines Development Campus , Severo Ochoa, 2 , 28760 Tres Cantos, Madrid , Spain.
  • Ferrer S; GlaxoSmithKline, Tres Cantos Medicines Development Campus , Severo Ochoa, 2 , 28760 Tres Cantos, Madrid , Spain.
  • Angulo-Barturen I; GlaxoSmithKline, Tres Cantos Medicines Development Campus , Severo Ochoa, 2 , 28760 Tres Cantos, Madrid , Spain.
  • Lafuente-Monasterio MJ; GlaxoSmithKline, Tres Cantos Medicines Development Campus , Severo Ochoa, 2 , 28760 Tres Cantos, Madrid , Spain.
  • Duffy J; GlaxoSmithKline, Tres Cantos Medicines Development Campus , Severo Ochoa, 2 , 28760 Tres Cantos, Madrid , Spain.
  • Burrows J; Medicines for Malaria Venture, ICC , Route de Pré-Bois 20 , PO Box 1826, 1215 Geneva , Switzerland.
  • Street LJ; Medicines for Malaria Venture, ICC , Route de Pré-Bois 20 , PO Box 1826, 1215 Geneva , Switzerland.
  • Chibale K; Drug Discovery and Development Center (H3D), Department of Chemistry , University of Cape Town , Rondebosch 7701 , South Africa.
J Med Chem ; 61(9): 4213-4227, 2018 05 10.
Article en En | MEDLINE | ID: mdl-29665687
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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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Plasmodium falciparum / Piridinas / Descubrimiento de Drogas / Imidazoles / Malaria Tipo de estudio: Diagnostic_studies Límite: Animals / Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2018 Tipo del documento: Article País de afiliación: Sudáfrica
Texto completo
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Plasmodium falciparum / Piridinas / Descubrimiento de Drogas / Imidazoles / Malaria Tipo de estudio: Diagnostic_studies Límite: Animals / Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2018 Tipo del documento: Article País de afiliación: Sudáfrica