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Synthesis and Evaluation of Nitroheterocyclic Aromatic Adamantanohydrazones with Trypanocidal Activity. Part III

Year: 2026

Type: article

Abstract: Extending our research on the design, synthesis, and pharmacological evaluation of antitrypanosomatid nitroheterocyclic aromatic adamantanes, we have identified hydrazone derivatives conjugated with 5-nitrothiophene that have submicromolar activity against trypanosomes. Key structural features, namely, the incorporation of the adamantane ring into the skeleton of the new compounds, the nature and the length of the hydrazone linker, and the nitroheterocycle moiety were evaluated to optimize both efficacy and safety profiles. It is also shown that these compounds function as prodrugs that are bioactivated by parasite-specific nitroreductase enzymes, primarily NTR-1. These findings suggest that nitroheterocyclic aromatic adamantanohydrazones represent promising candidates for further development as antitrypanosomal agents.

Source: ACS Infectious Diseases

DOI: 10.1021/acsinfecdis.6c00201

Authors: Angeliki-Sofia Foscolos, Konstantina Stavropoulou, Nuno Santarém, Anabela Cordeiro da Silva, Martin C. Taylor, Theodora Calogeropoulou, Andrew Tsotinis, Ioannis P. Papanastasiou, John M. Kelly, Susan Wyllie

Institutions: National and Kapodistrian University of Athens, National Centre of Scientific Research "Demokritos", Universidade do Porto, Department of Biological Sciences, i3S - Instituto de Investigação e Inovação em Saúde, Universidade do Porto, London School of Hygiene & Tropical Medicine, National Hellenic Research Foundation, University of Dundee

Language: English

Topic: Trypanosoma species research and implications

Subfield: Epidemiology

Field: Medicine

Domain: Health Sciences

SDG: Good health and well-being

Open Access status: hybrid

Estimated APC paid: $4,500

Funders: University of Dundee, Field Museum, Wellcome Trust, Hellenic Academic Libraries Link, European Cooperation in Science and Technology, Hellenic Foundation for Research and Innovation, Foundation for Science and Technology, Fundação para a Ciência e a Tecnologia

Awards: G3640454976, G4878332328, A platform for drug target deconvolution and exploitation, Centre for Neglected Tropical Diseases Drug Discovery, Centre for Neglected Tropical Diseases Drug Discovery, G5677973708, A platform for drug target deconvolution and exploitation

OpenAlex ID: W7165000418

FWCI:

Cites: 25

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