ArticleBioorganic & medicinal chemistry2014
Synthesis and antimalarial activity of metal complexes of cross-bridged tetraazamacrocyclic ligands.
Article in Bioorganic & medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 82 citations in OpenAlex.
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- A Bridge too Far? Comparison of Transition Metal Complexes of Dibenzyltetraazamacrocycles with and without Ethylene Cross-Bridges: X-ray Crystal Structures, Kinetic Stability, and Electronic Properties.Molecules (Basel, Switzerland) · 2023Article
- Bioorganometallic Compounds as Novel Drug Targets against Schistosomiasis in Sub-Saharan Africa: An alternative to Praziquantel?Advanced pharmaceutical bulletin · 2022Review
- Decrypting the Molecular Mechanistic Pathways Delineating the Chemotherapeutic Potential of Ruthenium-Phloretin Complex in Colon Carcinoma Correlated with the Oxidative Status and Increased Apoptotic Events.Oxidative medicine and cellular longevity · 2020Article
- Investigations into the Structure/Antibacterial Activity Relationships of Cyclam and Cyclen Derivatives.Antibiotics (Basel, Switzerland) · 2019Article
- Tetraazamacrocyclic derivatives and their metal complexes as antileishmanial leads.Polyhedron · 2019Article
- Mechanochemistry as an emerging tool for molecular synthesis: what can it offer?Chemical science · 2018Review
- Antiplasmodial activity of targeted zinc(II)-dipicolylamine complexes.Bioorganic & medicinal chemistry · 2017Article
- Some nontoxic metal-based drugs for selected prevalent tropical pathogenic diseases.Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry · 2017Review
- Discovery of Antischistosomal Drug Leads Based on Tetraazamacrocyclic Derivatives and Their Metal Complexes.Antimicrobial agents and chemotherapy · 2016Article
- Synthesis and structural studies of two pyridine-armed reinforced cyclen chelators and their transition metal complexes.Polyhedron · 2016Article
- Encapsulation of zinc-rifampicin complex into transferrin-conjugated silver quantum-dots improves its antimycobacterial activity and stability and facilitates drug delivery into macrophages.Scientific reports · 2016Article
Corrections and comments
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Authors and funding
12 authors at 4 institutions in 2 countries.
Funding
Abstract
Using transition metals such as manganese(II), iron(II), cobalt(II), nickel(II), copper(II), and zinc(II), several new metal complexes of cross-bridged tetraazamacrocyclic chelators namely, cyclen- and cyclam-analogs with benzyl groups, were synthesized and screened for in vitro antimalarial activity against chloroquine-resistant (W2) and chloroquine-sensitive (D6) strains of Plasmodium falciparum. The metal-free chelators tested showed little or no antimalarial activity. All the metal complexes of the dibenzyl cross-bridged cyclam ligand exhibited potent antimalarial activity. The Mn(2+) complex of this ligand was the most potent with IC50s of 0.127 and 0.157μM against the chloroquine-sensitive (D6) and chloroquine-resistant (W2) P. falciparum strains, respectively. In general, the dibenzyl hydrophobic ligands showed better anti-malarial activity compared to the activity of monobenzyl ligands, potentially because of their higher lipophilicity and thus better cell penetration ability. The higher antimalarial activity displayed by the manganese complex for the cyclam ligand in comparison to that of the cyclen, correlates with the larger pocket of cyclam compared to that of cyclen which produces a more stable complex with the Mn(2+). Few of the Cu(2+) and Fe(2+) complexes also showed improvement in activity but Ni(2+), Co(2+) and Zn(2+) complexes did not show any improvement in activity upon the metal-free ligands for anti-malarial development.
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Registered trials
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