ArticleMalaria journal2026
Searching for new candidates for antimalarial therapy: physicochemical and in vitro evaluation of gold(I) and silver(I) N-heterocyclic carbene complexes.
Article in Malaria journal, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
backgroundThe global fight against malaria is currently hindered by the rapid emergence and spread of multi-drug-resistant Plasmodium falciparum strains. This growing resistance has compromised the efficacy of frontline treatments and has led to the disease continuing to claim thousands of lives each year. Consequently, a new effective and non-toxic anti-malarial drug is urgently needed. In this context, metal-NHC (N-heterocyclic carbene) complexes have diverse physicochemical properties that could enhance biological activity and lead to the development of a new drug to combat malaria. On this regard, this study examined the biological activity of two metal-NHC complexes and their NHC precursor in two strains of the parasite, Plasmodium (3D7 and FCR-3), with specific targets.
methodsThe synthesis of all metal-NHC complexes was carried out under nitrogen atmosphere using Schlenk techniques. We studied the biological activity of two metal-NHC complexes and their NHC precursor in two Plasmodium strains (3D7 and FCR-3) and the selectivity index. Additionally, the possible interactions of these metal compounds with specific targets were evaluated. These targets included reactive oxygen species (ROS), albumin (BSA), Fe(III) PPIX, and β-hematin. The evaluation also included lipophilicity and ADMET properties. These properties were evaluated through diverse physical and spectroscopic methods.
resultsThe IC
conclusionsPreliminary studies reported in this paper suggest that the two metal-NHC complexes 1 and 2 interact with targets such as the inhibition of β-hematin and the production of reactive oxygen species (ROS). They also have lipophilic and physicochemical profiles that correlate with their antiplasmodial efficacy. Both complexes exhibit moderate activity, indicating potential for further evaluation. A plausible explanation is that this behavior arises from the nature of both the ligand and the metal center. Accordingly, these initial findings provide a basis for the further exploration of new antimalarial compounds.
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