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The preparation of the corresponding precursors included a series of transformations, such as haloperoxidation and Sonogashira cross\u2010coupling 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\u2010micromolar activity against intra\u2010erythrocytic forms of <jats:italic>Plasmodium falciparum<\/jats:italic>. The results from this hit\u2010to\u2010lead optimization are hereby reported for the first time.<\/jats:p>","DOI":"10.1002\/cmdc.202300264","type":"journal-article","created":{"date-parts":[[2023,7,1]],"date-time":"2023-07-01T11:47:59Z","timestamp":1688212079000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["Facile Access to Structurally Diverse Antimalarial Indoles Using a One\u2010Pot A<sup>3<\/sup> Coupling and Domino Cyclization Approach"],"prefix":"10.1002","volume":"18","author":[{"given":"Gustavo","family":"da Silva","sequence":"first","affiliation":[{"name":"Research Institute for Medicines (iMed.ULisboa) Faculdade de Farm\u00e1cia da Universidade de Lisboa  Av. Prof. Gama Pinto 1649-003 Lisboa Portugal"},{"name":"LAQV-REQUIMTE and Department of Chemistry University of Aveiro  Campus Universit\u00e1rio de Santiago 3810-193 Aveiro Portugal"}]},{"given":"Andr\u00e9 F. S.","family":"Luz","sequence":"additional","affiliation":[{"name":"Research Institute for Medicines (iMed.ULisboa) Faculdade de Farm\u00e1cia da Universidade de Lisboa  Av. Prof. Gama Pinto 1649-003 Lisboa Portugal"}]},{"given":"Denise","family":"Duarte","sequence":"additional","affiliation":[{"name":"GHTM \u2013 Global Health and Tropical Medicine Universidade Nova de Lisboa  Rua da Junqueira n\u00b0\u2005100 1349-008 Lisboa Portugal"}]},{"given":"Diana","family":"Fontinha","sequence":"additional","affiliation":[{"name":"Instituto de Medicina Molecular Faculdade de Medicina Universidade de Lisboa  Av. Prof. Egas Moniz 1649-028 Lisboa Portugal"}]},{"given":"Vera L. 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