ArticleMolecules (Basel, Switzerland)2016
Antileishmanial Activity and Structure-Activity Relationship of Triazolic Compounds Derived from the Neolignans Grandisin, Veraguensin, and Machilin G.
Article in Molecules (Basel, Switzerland), 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed.
- New Copper (II) Complexes Based on 1,4-Disubstituted-1,2,3-Triazole Ligands with Promising Antileishmanial Activity.Pharmaceutics · 2026Article
- Recent advances in structural modifications of natural products for anti-leishmaniasis therapy (2010-2024).RSC medicinal chemistry · 2025Review
- Article
- Insights into the current status of privileged N-heterocycles as antileishmanial agents.Molecular diversity · 2020Review
- A Triazole Hybrid of Neolignans as a Potential Antileishmanial Agent by Triggering Mitochondrial Dysfunction.Molecules (Basel, Switzerland) · 2019Article
- Second-generation pterocarpanquinones: synthesis and antileishmanial activity.The journal of venomous animals and toxins including tropical diseases · 2018Article
- In Vitro antileishmania activity of sesquiterpene-rich essential oils from Nectandra species.Pharmaceutical biology · 2017Article
- The Structure-Antimicrobial Activity Relationships of a Promising Class of the Compounds Containing the N-Arylpiperazine Scaffold.Molecules (Basel, Switzerland) · 2016Article
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Authors and funding
10 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Sixteen 1,4-diaryl-1,2,3-triazole compounds 4-19 derived from the tetrahydrofuran neolignans veraguensin 1, grandisin 2, and machilin G 3 were tested against Leishmania (Leishmania) amazonensis intracellular amastigotes. Triazole compounds 4-19 were synthetized via Click Chemistry strategy by 1,3-dipolar cycloaddition between terminal acetylenes and aryl azides containing methoxy and methylenedioxy groups as substituents. Our results suggest that most derivatives were active against intracellular amastigotes, with IC50 values ranging from 4.4 to 32.7 µM. The index of molecular hydrophobicity (ClogP) ranged from 2.8 to 3.4, reflecting a lipophilicity/hydrosolubility rate suitable for transport across membranes, which may have resulted in the potent antileishmanial activity observed. Regarding structure-activity relationship (SAR), compounds 14 and 19, containing a trimethoxy group, were the most active (IC50 values of 5.6 and 4.4 µM, respectively), with low cytotoxicity on mammalian cells (SI = 14.1 and 10.6). These compounds induced nitric oxide production by the host macrophage cells, which could be suggested as the mechanism involved in the intracellular killing of parasites. These results would be useful for the planning of new derivatives with higher antileishmanial activities.
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