ArticleAntimicrobial agents and chemotherapy2012
Novel potent metallocenes against liver stage malaria.
Article in Antimicrobial agents and chemotherapy, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 34 citations in OpenAlex.
- Harmicens, Novel Harmine and Ferrocene Hybrids: Design, Synthesis and Biological Activity.International journal of molecular sciences · 2022Article
- A New Thienopyrimidinone Chemotype Shows Multistage Activity against Plasmodium falciparum, Including Artemisinin-Resistant Parasites.Microbiology spectrum · 2021Article
- Enhancing the Activity of Drugs by Conjugation to Organometallic Fragments.Chemistry (Weinheim an der Bergstrasse, Germany) · 2020Review
- Insights into the current status of privileged N-heterocycles as antileishmanial agents.Molecular diversity · 2020Review
- Coupling the Antimalarial Cell Penetrating Peptide TP10 to Classical Antimalarial Drugs Primaquine and Chloroquine Produces Strongly Hemolytic Conjugates.Molecules (Basel, Switzerland) · 2019Article
- Primaquine derivatives: Modifications of the terminal amino group.European journal of medicinal chemistry · 2019Review
- Coupling the cell-penetrating peptides transportan and transportan 10 to primaquine enhances its activity against liver-stage malaria parasites.MedChemComm · 2019Article
- Chloroquine Analogues as Leads against Pneumocystis Lung Pathogens.Antimicrobial agents and chemotherapy · 2018Article
- Differential activity of methylene blue against erythrocytic and hepatic stages of Plasmodium.Malaria journal · 2018Article
- Peptidomimetic and organometallic derivatives of primaquine active against Leishmania infantum.Antimicrobial agents and chemotherapy · 2012Article
Corrections and comments
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Authors and funding
10 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Novel conjugates of the antimalarial drug primaquine (compound 1) with ferrocene, named primacenes, have been synthesized and screened for their activities against blood stage and liver stage malaria in vitro and host-vector transmission in vivo. Both transmission-blocking and blood-schizontocidal activities of the parent drug were conserved only in primacenes bearing a basic aliphatic amine group. Liver stage activity did not require this structural feature, and all metallocenes tested were comparable to or better than primaquine in this regard. Remarkably, the replacement of primaquine's aliphatic chain by hexylferrocene, as in compound 7, led to a ~45-fold-higher level activity against liver stage parasitemia than that of primaquine.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.