ArticleACS infectious diseases2018
Small Molecule Inhibitors of Metabolic Enzymes Repurposed as a New Class of Anthelmintics.
Article in ACS infectious diseases, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 26 citations in OpenAlex.
- Design, synthesis, and biological evaluation of a focused pyrrolo- and pyrido-quinazolinone natural products-templated library for anti-fungal and anthelmintic activities.Bioorganic & medicinal chemistry · 2026Article
- Discovery of novel repurposed anthelminthics againstCurrent research in parasitology & vector-borne diseases · 2026Article
- Discovery of Human PIM Kinase Inhibitors as a Class of Anthelmintic Drugs to Treat Intestinal Nematode Infections.ACS infectious diseases · 2025Article
- High-Throughput Screening of More Than 30,000 Compounds for Anthelmintics against Gastrointestinal Nematode Parasites.ACS infectious diseases · 2025Article
- Article
- Multivariate chemogenomic screening prioritizes new macrofilaricidal leads.Communications biology · 2023Article
- Parasite OMICS, the grand challenges ahead.Frontiers in parasitology · 2022Article
- Structural Requirements for Dihydrobenzoxazepinone Anthelmintics: Actions against Medically Important and Model Parasites:ACS infectious diseases · 2021Article
- Areas of Metabolomic Exploration for Helminth Infections.ACS infectious diseases · 2021Article
- Rapid determination of nematode cell and organ susceptibility to toxic treatments.International journal for parasitology. Drugs and drug resistance · 2020Article
- Profiling microRNAs through development of the parasitic nematode Haemonchus identifies nematode-specific miRNAs that suppress larval development.Scientific reports · 2019Article
- Drug Screening for Discovery of Broad-spectrum Agents for Soil-transmitted Nematodes.Scientific reports · 2019Article
- Identification of small molecule enzyme inhibitors as broad-spectrum anthelmintics.Scientific reports · 2019Article
- A highly expressed intestinal cysteine protease of Ancylostoma ceylanicum protects vaccinated hamsters from hookworm infection.PLoS neglected tropical diseases · 2019Article
Corrections and comments
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Authors and funding
18 authors at 7 institutions in 2 countries.
Funding
Abstract
The enormous prevalence of infections caused by parasitic nematodes worldwide, coupled to the rapid emergence of their resistance to commonly used anthelmintic drugs, presents an urgent need for the discovery of new drugs. Herein, we have identified several classes of small molecules with broad spectrum activity against these pathogens. Previously, we reported the identification of carnitine palmitoyltransferases (CPTs) as a representative class of enzymes as potential targets for metabolic chokepoint intervention that was elucidated from a combination of chemogenomic screening and experimental testing in nematodes. Expanding on these previous findings, we have discovered that several chemical classes of known small molecule inhibitors of mammalian CPTs have potent activity as anthelmintics. Cross-clade efficacy against a broad spectrum of adult parasitic nematodes was demonstrated for multiple compounds from different series. Several analogs of these initial hit compounds were designed and synthesized. The compounds we report represent a good starting point for further lead identification and optimization for development of new anthelmintic drugs with broad spectrum activity and a novel mechanism of action.
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Registered trials
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