<![CDATA[Malaria caused by Plasmodium falciparum remains a health problem due to increasing resistance to antimalarial drugs, including artemisinin-based therapy. This study aims to examine the potential and strategies for molecular modification of bioactive compounds in medicinal plants as effective and safe new antimalarial candidates. The method used was a descriptive-qualitative literature review of 19 scientific articles published in 2011–2026 and obtained from Google Scholar, PubMed, and ScienceDirect. The results of the study indicate that plants such as Momordica charantia, Fraxinus griffithii, Piper sulcatum, and Eucalyptus globulus contain secondary metabolites in the form of alkaloids, flavonoids, and terpenoids that have potential as antiplasmodials. Chemical modifications, such as methylation, acetylation, and esterification, supported by in silico modeling and biological tests can improve the stability, affinity, bioavailability, and selectivity of compounds. Thus, molecular modification based on structure-activity relationship (SAR) has the potential to be a strategy for developing new antimalarial drug candidates to address drug resistance.]]>
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