Detalhes bibliográficos
| Resumo: | A multistep and diversity-oriented synthetic route aiming at the A3 coupling/domino cyclization of o-ethynyl anilines, aldehydes and s-amines is described. The preparation of the corresponding precursors included a series of transformations, such as haloperoxidation and Sonogashira cross-coupling reactions, amine protection, desilylation and amine reduction. Some products of the multicomponent reaction underwent further detosylation and Suzuki coupling. The resulting library of structurally diverse compounds was evaluated against blood and liver stage malaria parasites, which revealed a promising lead with sub-micromolar activity against intra-erythrocytic forms of Plasmodium falciparum. The results from this hit-to-lead optimization are hereby reported for the first time. |
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| Autores principais: | Silva, Gustavo Da |
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| Outros Autores: | Luz, André F. S.; Duarte, Denise; Fontinha, Diana; Silva, Vera L. M.; Almeida Paz, Filipe A.; Madureira, Ana Margarida; Simões, Sandra; Prudêncio, Miguel; Nogueira, Fátima; Silva, Artur M. S.; Moreira, Rui |
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| Assunto: | A3 coupling Antimalarials Indoles Multicomponent reactions One-pot synthesis |
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| Ano: | 2023 |
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| País: | Portugal |
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| Tipo de documento: | artigo |
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| Tipo de acesso: | acesso restrito |
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| Instituição associada: | Universidade de Lisboa |
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| Idioma: | inglês |
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| Origem: | Repositório da Universidade de Lisboa |
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