ArticleChemMedChem2019
Discovery of Sustainable Drugs for Neglected Tropical Diseases: Cashew Nut Shell Liquid (CNSL)-Based Hybrids Target Mitochondrial Function and ATP Production in Trypanosoma brucei.
Article in ChemMedChem, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed.
- Synthesis of Isochromans From Anacardic Acids Obtained From Cashew Nutshell Liquid (CNSL) and Their Antimicrobial Activity.Chemistry & biodiversity · 2026Article
- The many facets of sustainability in medicinal chemistry: our personal experience.RSC medicinal chemistry · 2026Article
- Evaluation of the trypanocidal and immunomodulatory effects of LDT409, a cardanol derivative from cashew nut shell liquid.Frontiers in immunology · 2026Article
- Inhibitory Activity of LDT10 and LDT119, New Saturated Cardanols, AgainstPharmaceuticals (Basel, Switzerland) · 2025Article
- Sustainable Antiparasitic Agents from an Agro-Industrial Waste: Mitochondria-Targeting Cashew Nutshell Liquid-Derived Phosphonium and Ammonium Salts.Journal of medicinal chemistry · 2025Article
- Benign-by-Design SAHA Analogues for Human and Animal Vector-Borne Parasitic Diseases.ACS medicinal chemistry letters · 2024Article
- Harnessing the 12 Green Chemistry Principles for Sustainable Antiparasitic Drugs: Toward the One Health Approach.ACS infectious diseases · 2024Review
- Article
- Discovery of sustainable drugs for Alzheimer's disease: cardanol-derived cholinesterase inhibitors with antioxidant and anti-amyloid properties.RSC medicinal chemistry · 2021Article
- Antitrypanosomal and Antileishmanial Activity of Chalcones and Flavanones fromPathogens (Basel, Switzerland) · 2021Article
- Novel flavanones with anti-trypanosomal activity isolated from Zambian and Tanzanian propolis samples.International journal for parasitology. Drugs and drug resistance · 2020Article
- Chlorinated plastoquinone analogs that inhibit Staphylococcus epidermidis and Candida albicans growth.Folia microbiologica · 2020Article
- Investigation of 5'-Norcarbocyclic Nucleoside Analogues as Antiprotozoal and Antibacterial Agents.Molecules (Basel, Switzerland) · 2019Article
- European propolis is highly active against trypanosomatids including Crithidia fasciculata.Scientific reports · 2019Article
- Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease.ACS medicinal chemistry letters · 2019Article
- Article
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Authors and funding
12 authors.
Funding
Abstract
In the search for effective and sustainable drugs for human African trypanosomiasis (HAT), we developed hybrid compounds by merging the structural features of quinone 4 (2-phenoxynaphthalene-1,4-dione) with those of phenolic constituents from cashew nut shell liquid (CNSL). CNSL is a waste product from cashew nut processing factories, with great potential as a source of drug precursors. The synthesized compounds were tested against Trypanosoma brucei brucei, including three multidrug-resistant strains, T. congolense, and a human cell line. The most potent activity was found against T. b. brucei, the causative agent of HAT. Shorter-chain derivatives 20 (2-(3-(8-hydroxyoctyl)phenoxy)-5-methoxynaphthalene-1,4-dione) and 22 (5-hydroxy-2-(3-(8-hydroxyoctyl)phenoxy)naphthalene-1,4-dione) were more active than 4, displaying rapid micromolar trypanocidal activity, and no human cytotoxicity. Preliminary studies probing their mode of action on trypanosomes showed ATP depletion, followed by mitochondrial membrane depolarization and mitochondrion ultrastructural damage. This was accompanied by reactive oxygen species production. We envisage that such compounds, obtained from a renewable and inexpensive material, might be promising bio-based sustainable hits for anti-trypanosomatid drug discovery.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.