Parasitic nematodes are amongst the most prevalent disease-causing agents of humans, livestock, and companion animals. Soil-Transmitted Nematodes (STN), namely hookworms, whipworms, and ascarids, are extremely common parasites, infecting 1–2 billion of the poorest people worldwide mostly living in tropical countries. Many fungicidal drugs were found to have potent and broad-spectrum anthelmintic activity among those are sulconazole, econazole, miconazole, and clotrimazole The objective of my capstone undergraduate research project is to synthesize antifungal and antihelminthic compounds based off of a natural compound, Lutonin that has been extracted from <i>Peganum Nigellastrum</i>.  The similarity in drug susceptibility between nematode parasites and fungal pathogens could be explained by the process of convergent evolution of structurally and functionally similar and indispensable targets essential for the process of parasitism facing similar conditions in vertebrate hosts. Because STNs are not amenable to high-throughput screening and require laboratory animals for maintenance, not to mention the associated costs, we propose to use pathogenic fungi, amenable to high-throughput screening, as a primary screening model followed by secondary screening against parasitic nematodes. Our approach will increase and maximize the outputs of a single drug screening project with the ability to identify leads with fungicidal and/or anthelmintic activity.   The details of the synthesis of luotonin analogs and screening progress will be shared.

Generation of luotonin based leads for anti-fungal and anti-helminthis purposes

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ACS Fall 2022

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