Chemical modification of monensin as a source of potent antiplasmodial agents

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dc.contributor.authorSulik, Michał
dc.contributor.authorWorkneh, Eyob
dc.contributor.authorSantana, Sofia
dc.contributor.authorTeixeira, Bárbara
dc.contributor.authorPrudêncio, Miguel
dc.contributor.authorJanczak, Jan
dc.contributor.authorHuczyński, Adam
dc.contributor.organizationDepartment of Medical Chemistry, Faculty of Chemistry, Adam Mickiewicz University,Poznań, Poland
dc.contributor.organizationGIMM - Gulbenkian Institute for Molecular Medicine, Lisboa, Portugal
dc.contributor.organizationFaculdade de Medicina da Universidade de Lisboa, Lisboa, Portugal
dc.contributor.organizationInstitute of Low Temperature and Structure Research, Polish Academy of Sciences, Wrocław, Poland
dc.date.accessioned2025-04-01T06:30:04Z
dc.date.available2025-04-01T06:30:04Z
dc.date.issued2025-03-26
dc.description.abstractMalaria remains a significant public health issue and one of the leading causes of child mortality worldwide. Due to the growing problem of drug resistance, new modes of fighting the disease are searched for. In this context, ionophore antibiotics, natural compounds with high potential for combating parasitic diseases, deserve special attention. The primary representative of such compounds, monensin (MON), demonstrates exceptionally high antiplasmodial activity. In this work, the C26-amino derivative of MON was used as a convenient substrate for the synthesis of its acyl analogues, such as amides and urea. All derivatives exhibited strong activity against the hepatic stage of Plasmodium berghei infection in vitro, which exceeded that shown by the reference drug primaquine. The IC50 value for MON O-phenyl urethane (8) was less than 1 nM.en
dc.description.sponsorshipThis research was financially supported by an OPUS 21 grant (2021/41/B/ST4/00088) funded to A.H. by the National Science Center in Poland (NCN). For the purpose of Open Access, the authors have applied public copyright license to any Author Accepted Manuscript (AAM) version arising from this submission.
dc.identifier.citationM. Sulik, E.A. Workneh, S. Santana, B. Teixeira, M. Prudêncio, J. Janczak, A. Huczyński, Chemical modification of monensin as a source of potent antiplasmodial agents, Bioorganic & Medicinal Chemistry (2025), doi: https://doi.org/10.1016/j.bmc.2025.118177
dc.identifier.doi10.1016/j.bmc.2025.118177
dc.identifier.urihttps://open.icm.edu.pl/handle/123456789/25586
dc.language.isoen
dc.publisherElsevier
dc.rightsUznanie autorstwa 4.0 Międzynarodoween
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/
dc.sourceBioorganic & Medicinal Chemistry
dc.subjectionophoresen
dc.subjectplasmodium bergheien
dc.subjectantiplasmodial activityen
dc.subjectmalariaen
dc.titleChemical modification of monensin as a source of potent antiplasmodial agentsen
dc.typearticle
dc.type.versionpublishedVersion
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