Development of a synthetic route towards N4,N9-disubstituted 4,9-diaminoacridines: On the way to multi-stage antimalarials |
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Authors: | Mélanie Fonte Natália Fagundes Ana Gomes Ricardo Ferraz Cristina Prudêncio Maria João Araújo Paula Gomes Cátia Teixeira |
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Affiliation: | 1. LAQV-REQUIMTE, Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade do Porto, P-4169-007 Porto, Portugal;2. Ciências Químicas e das Biomoléculas, Escola Superior de Saúde, Politécnico do Porto, P-4200-072 Porto, Portugal;3. i3S – Instituto de Investigação e Inovação em Saúde da Universidade do Porto, P-4200-393 Porto, Portugal |
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Abstract: | A multi-step synthetic route towards N4,N9-disubstituted 4,9-diaminoacridines that, to the best of our knowledge, has no precedence in the literature, has been developed. The target structures are likely to reveal interesting biological activities in the near future, not only due to their mepacrine-like core, but also because they embed simultaneously the pharmacophores of chloroquine and primaquine, antimalarial drugs that act at different stages of malaria infection. |
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Keywords: | Acridine Antimalarial Heteroaromatic Heterocyclic chemistry Mepacrine Quinacrine |
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