Aug 2026· ACS Omega· Vol 11, pp. 49026 - 49032· 0 citations· 48 references
Medicine
TL;DR
Based on the known antileishmanial properties of eugenol and its derivatives, a series of novel disubstituted 1,2,3-triazoles was prepared via the classical 1,3-dipolar cycloaddition reaction, employing a eugenol-azide derivative, and emerged as the most active molecule.
Abstract
Among tropical neglected diseases, leishmaniasis stands out. This parasitic infection occurs in numerous countries, affecting thousands of people worldwide. The currently available therapies present important limitations, including high toxicity, long treatment periods requiring parenteral administration, and the emergence of parasite resistance. Based on the known antileishmanial properties of eugenol and its derivatives, a series of novel disubstituted 1,2,3-triazoles was prepared via the classical 1,3-dipolar cycloaddition reaction, employing a eugenol-azide derivative. These compounds were subsequently evaluated against Leishmania amazonensis (promastigotes and amastigotes). Compound 4d emerged as the most active molecule in the series, exhibiting an IC50 = 3.98 ± 1.05 μM against amastigotes and a selectivity index greater than 50.25, thereby retaining and even enhancing the antileishmanial activity of its natural-product precursor.
Given the reluctance of pharmaceutical companies to invest in new antileishmanial drugs, due to high costs and low perspectives of financial return, there is growing interest in repurposing existing drugs, often a more cost‐effective and quicker strategy to launch effective therapeutic solutions. Artemisinins, used as...
Inês C. C. Costa, Patrícia S. M. Amado, Philippe M. Loiseau et al.· ChemMedChem· 0 citations
Leishmaniasis is a neglected tropical disease with a devastating global impact. The current medications on the market for treating this protozoan parasitic infection are insufficient to fit the global need, with long durations of therapy, growing resistance rates, and severe adverse effects. This investigation aims t...
Lucas Daut, Jonathan Taylor, Nicola S. Carter et al.· Frontiers in Pharmacology· 0 citations
Chagas disease and leishmaniasis are neglected tropical diseases with limited treatment options. This study reports a hit‐to‐lead optimization of morpholinephenylbenzamides, starting from hit 1, which showed potent activity against Trypanosoma cruzi (IC50 0.29–0.76 μM) and Leishmania infantum (IC50 10.7 μM), despite a...
D. Farago, Daniela de Melo Resende, Mariza Gabriela Faleiro de Moura Lodi Cruz et al.· ChemMedChem· 0 citations
Kinetoplastid diseases remain a major global health challenge, highlighting the need for new antiparasitic chemotypes.
N,N′
-disubstituted aliphatic diamines have emerged as a promising scaffold against trypanosomatid parasites. Building on our previous studies, we expanded the structure–activity relationship (SAR)...
Alejandro I. Recio-Balsells, Esteban A. Panozzo-Zénere, E. Coser et al.· Frontiers in Chemical Biolog...· 0 citations
American Tegumentary Leishmaniasis, primarily caused by Leishmania (Viannia) braziliensis, remains a major public health challenge in Latin America. The variable efficacy and toxicity of pentavalent antimonials underscore the urgent need for new therapeutic candidates. Among the compounds currently explored, chalcone...
Edgar Schaeffer, G. Dias-Lopes, Patrícia Queiroz Monteiro et al.· ACS Omega· 0 citations
This study presents a comparative in vitro evaluation of 24 natural sesquiterpene γ-lactones and selected semisynthetic derivatives against three trypanosomatid parasites responsible for neglected tropical diseases: Trypanosoma brucei brucei, Trypanosoma cruzi, and Leishmania amazonensis. The compounds were screened fo...
S. Adekenov, L. Laurella, S. Sergazy et al.· International Journal of Mol...· 0 citations
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