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Novel Benzofuranyl Chalcones With Antileishmanial Activity: Synthesis, Structure-Activity Relationships, and
Adrián Durán-Vargas1,2, Enrique García-Hernández2, Gabriela Torres-Santiago1
1Facultad de Ciencias Químicas, Universidad Autónoma de Chihuahua, Chihuahua, Chihuahua, México.
Chemmedchem
|July 21, 2026
Summary
Researchers developed novel benzofuranyl chalcones as potential treatments for leishmaniasis. The most effective compound, 14l, showed significant antileishmanial activity with low toxicity to host cells.
Area of Science:
- Medicinal Chemistry
- Parasitology
- Drug Discovery
Background:
- Leishmaniasis is a neglected tropical disease requiring new drug candidates.
- Existing treatments face challenges like resistance and toxicity.
- Selective antileishmanial chemotypes are urgently needed.
Purpose of the Study:
- To design, synthesize, and evaluate benzofuranyl chalcones as antileishmanial agents.
- To identify potent and selective compounds against Leishmania mexicana.
- To explore structure-activity relationships for optimizing antileishmanial activity.
Main Methods:
- Synthesis of two series of benzofuranyl chalcone derivatives.
- Primary screening of compounds against L. mexicana at 5 µg/mL.
- Dose-response studies to determine IC50 values.
- Cytotoxicity assays using J774A.1 murine macrophages.
- Computational docking studies.
Main Results:
- 25 compounds inhibited parasite metabolism by over 50% in primary screening.
- Compound 14l emerged as the most potent analog with an IC50 of 2.1 µM.
- Several other compounds demonstrated low-micromolar activity (IC50 < 5 µM).
- Prioritized compounds exhibited high selectivity indices (SI > 666.7 for 14l).
- Structure-activity relationship analysis revealed key substituent effects.
Conclusions:
- Benzofuranyl chalcones represent a promising scaffold for developing new antileishmanial drugs.
- Compound 14l is a lead candidate for further investigation.
- Optimized substitution patterns enhance antileishmanial potency and selectivity.
- Further studies are needed to validate the proposed mechanism of action.
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