Antimalarial Pyrido[1,2- a]benzimidazole Derivatives with Mannich Base Side Chains: Synthesis, Pharmacological Evaluation, and Reactive Metabolite Trapping Studies.

Okombo, John; Brunschwig, Christel; Singh, Kawaljit; Dziwornu, Godwin Akpeko; Barnard, Linley; Njoroge, Mathew; Wittlin, Sergio; Chibale, Kelly

Okombo, John; Brunschwig, Christel; Singh, Kawaljit; Dziwornu, Godwin Akpeko; Barnard, Linley; Njoroge, Mathew; Wittlin, Sergio; Chibale, Kelly.

Afiliação

Okombo J; Department of Chemistry , University of Cape Town , Rondebosch 7701 , South Africa.
Brunschwig C; Drug Discovery and Development Centre (H3D), Division of Clinical Pharmacology, Department of Medicine , University of Cape Town , Observatory 7925 , South Africa.
Singh K; South African Medical Research Council Drug Discovery and Development Research Unit, Department of Chemistry , University of Cape Town , Rondebosch 7701 , South Africa.
Dziwornu GA; Department of Chemistry , University of Cape Town , Rondebosch 7701 , South Africa.
Barnard L; Department of Chemistry , University of Cape Town , Rondebosch 7701 , South Africa.
Njoroge M; Drug Discovery and Development Centre (H3D), Division of Clinical Pharmacology, Department of Medicine , University of Cape Town , Observatory 7925 , South Africa.
Wittlin S; Swiss Tropical and Public Health Institute , Socinstrasse 57 , Basel 4002 , Switzerland.
Chibale K; University of Basel , Basel 4003 , Switzerland.

ACS Infect Dis ; 5(3): 372-384, 2019 03 08.

Article em En | MEDLINE | ID: mdl-30608648

Assuntos

Antimaláricos/administração & dosagem; Antimaláricos/química; Benzimidazóis/administração & dosagem; Benzimidazóis/química; Malária/tratamento farmacológico; Bases de Mannich/química; Plasmodium falciparum/efeitos dos fármacos; Animais; Antimaláricos/síntese química; Antimaláricos/farmacocinética; Benzimidazóis/síntese química; Benzimidazóis/farmacocinética; Avaliação Pré-Clínica de Medicamentos; Humanos; Malária/parasitologia; Masculino; Camundongos; Camundongos Endogâmicos BALB C; Plasmodium berghei; Plasmodium falciparum/fisiologia; Relação Estrutura-Atividade

Palavras-chave

4-aminophenol; Mannich base; Plasmodium falciparum; amodiaquine; pyrido[1,2-a]benzimidazoles; reactive metabolite

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Plasmodium falciparum / Benzimidazóis / Malária / Bases de Mannich / Antimaláricos Limite: Animals / Humans / Male Idioma: En Ano de publicação: 2019 Tipo de documento: Article

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