ArticlePloS one2024
Exploring hydrophilic 2,2-di(indol-3-yl)ethanamine derivatives against Leishmania infantum.
Article in PloS one, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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Who cites it
4 citing papers in PubMed.
- Arylation of Olefins with N-Unprotected Bromobisindole Ethanamines: Expanding the Scope of the Mizoroki-Heck Reaction.The Journal of organic chemistry · 2026Article
- Article
- Efficient and Rapid Arylation of NH₂-Unprotected Bromobisindole Ethanamines via Suzuki-Miyaura Coupling: Generating New Leads Against Leishmania.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- Easy one-pot synthesis of multifunctionalized indole-pyrrole hybrids as a new class of antileishmanial agents.RSC advances · 2024Article
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Authors and funding
11 authors.
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Abstract
Herein we report the design and the synthesis of a library of new and more hydrophilic bisindole analogues based on our previously identified antileishmanial compound URB1483 that failed the preliminary in vivo test. The novel bisindoles were phenotypically screened for efficacy against Leishmania infantum promastigotes and simultaneously for toxicity on human macrophage-like THP-1 cells. Among the less toxic compounds, eight bisindoles showed IC50 below 10 μM. The most selective compound 1h (selectivity index = 10.1, comparable to miltefosine) and the most potent compound 2c (IC50 = 2.7 μM) were tested for their efficacy on L. infantum intracellular amastigotes. The compounds also demonstrated their efficacy in the in vitro infection model, showing IC50 of 11.1 and 6.8 μM for 1h and 2c, respectively. Moreover, 1h showed a better toxicity profile than the commercial drug miltefosine. For all these reasons, 1h could be a possible new starting point for hydrophilic antileishmanial agents with low cytotoxicity on human macrophage-like cells.
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