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In this study, we realized a library of novel bisindole derivatives as potential antileishmanial agents through a rapid Suzuki\u2010Miyaura coupling reaction, utilizing NH<jats:sub>2<\/jats:sub>\u2010unprotected bromobisindole ethanamines and boronic acids. Optimization of reaction conditions allowed for the efficient and selective arylation of these substrates, with yields up to 93%. The compounds were screened for their activity against <jats:italic>Leishmania infantum<\/jats:italic> promastigotes. Among the tested bisindole derivatives, <jats:bold>3af<\/jats:bold> (bearing a 4\u2010vinylphenyl moiety) demonstrated potent antileishmanial activity (IC<jats:sub>50<\/jats:sub> = 1.1 \u00b5M) with a higher selectivity index (21.8) compared to the reference drug miltefosine (9.8). A significant activity was also retained against intracellular amastigotes. This study establishes a robust methodology for late\u2010stage functionalization of bisindoles, also highlighting these derivatives' potential as promising leads for antileishmanial drug development.<\/jats:p>","DOI":"10.1002\/chem.202500637","type":"journal-article","created":{"date-parts":[[2025,5,9]],"date-time":"2025-05-09T07:24:04Z","timestamp":1746775444000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["Efficient and Rapid Arylation of NH\u2082\u2010Unprotected Bromobisindole Ethanamines via Suzuki\u2010Miyaura Coupling: Generating New Leads Against <i>Leishmania<\/i>"],"prefix":"10.1002","volume":"31","author":[{"given":"Alessandro","family":"Buono","sequence":"first","affiliation":[{"name":"Department of Biomolecular Sciences Section of Chemistry and Pharmaceutical Technologies University of Urbino Carlo Bo  Campus Scientifico E. 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