scholarly journals Comparison of the susceptibility of Plasmodium knowlesi and Plasmodium falciparum to antimalarial agents

2017 ◽  
Vol 72 (11) ◽  
pp. 3051-3058 ◽  
Author(s):  
Donelly A van Schalkwyk ◽  
Robert W Moon ◽  
Benjamin Blasco ◽  
Colin J Sutherland
Keyword(s):  
Plasmodium Falciparum ◽  
Plasmodium Knowlesi ◽  
Antimalarial Agents

The development of quinoloneesters as novel antimalarial agents targeting the Plasmodium falciparum bc1protein complex

MedChemComm ◽  
2012 ◽  
Vol 3 (1) ◽  
pp. 39-44 ◽  
Author(s):  
Robin Cowley ◽  
Suet Leung ◽  
Nicholas Fisher ◽  
Mohammed Al-Helal ◽  
Neil G. Berry ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Antimalarial Agents

Specific Inhibitors of Plasmodium falciparum Thioredoxin Reductase as Potential Antimalarial Agents.

ChemInform ◽  
2006 ◽  
Vol 37 (30) ◽  
Author(s):  
A. D. Adricopulo ◽  
M. B. Akoachere ◽  
R. Krogh ◽  
C. Nickel ◽  
M. J. McLeish ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Thioredoxin Reductase ◽  
Antimalarial Agents ◽  
Specific Inhibitors

scholarly journals Boromycin has Rapid-Onset Antibiotic Activity Against Asexual and Sexual Blood Stages of Plasmodium falciparum

2022 ◽  
Vol 11 ◽  
Author(s):  
Laís Pessanha de Carvalho ◽  
Sara Groeger-Otero ◽  
Andrea Kreidenweiss ◽  
Peter G. Kremsner ◽  
Benjamin Mordmüller ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Plasmodium Knowlesi ◽  
Rapid Onset ◽  
Multidrug Resistant ◽  
Antiplasmodial Activity ◽  
Onset Of Action ◽  
Streptomyces Antibioticus ◽  
Life Cycle Stages ◽  
Almost All

Boromycin is a boron-containing macrolide antibiotic produced by Streptomyces antibioticus with potent activity against certain viruses, Gram-positive bacteria and protozoan parasites. Most antimalarial antibiotics affect plasmodial organelles of prokaryotic origin and have a relatively slow onset of action. They are used for malaria prophylaxis and for the treatment of malaria when combined to a fast-acting drug. Despite the success of artemisinin combination therapies, the current gold standard treatment, new alternatives are constantly needed due to the ability of malaria parasites to become resistant to almost all drugs that are in heavy clinical use. In vitro antiplasmodial activity screens of tetracyclines (omadacycline, sarecycline, methacycline, demeclocycline, lymecycline, meclocycline), macrolides (oleandomycin, boromycin, josamycin, troleandomycin), and control drugs (chloroquine, clindamycin, doxycycline, minocycline, eravacycline) revealed boromycin as highly potent against Plasmodium falciparum and the zoonotic Plasmodium knowlesi. In contrast to tetracyclines, boromycin rapidly killed asexual stages of both Plasmodium species already at low concentrations (~ 1 nM) including multidrug resistant P. falciparum strains (Dd2, K1, 7G8). In addition, boromycin was active against P. falciparum stage V gametocytes at a low nanomolar range (IC50: 8.5 ± 3.6 nM). Assessment of the mode of action excluded the apicoplast as the main target. Although there was an ionophoric activity on potassium channels, the effect was too low to explain the drug´s antiplasmodial activity. Boromycin is a promising antimalarial candidate with activity against multiple life cycle stages of the parasite.

scholarly journals Use of a highly specific kinase inhibitor for rapid, simple and precise synchronization of Plasmodium falciparum and Plasmodium knowlesi asexual blood-stage parasites

PLoS ONE ◽  
2020 ◽  
Vol 15 (7) ◽  
pp. e0235798
Author(s):  
Margarida Ressurreição ◽  
James A. Thomas ◽  
Stephanie D. Nofal ◽  
Christian Flueck ◽  
Robert W. Moon ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Kinase Inhibitor ◽  
Plasmodium Knowlesi ◽  
Blood Stage ◽  
Asexual Blood Stage ◽  
Specific Kinase Inhibitor

Immunogenic Antigens Common to Plasmodium knowlesi and Plasmodium falciparum Are Expressed on the Surface of Infected Erythrocytes

1982 ◽  
Vol 68 (2) ◽  
pp. 185 ◽  
Author(s):  
Rupert Schmidt-Ullrich ◽  
Louis H. Miller ◽  
Donald F. H. Wallach ◽  
John Lightholder
Keyword(s):  
Plasmodium Falciparum ◽  
Plasmodium Knowlesi

scholarly journals Artemisone and Artemiside Are Potent Panreactive Antimalarial Agents That Also Synergize Redox Imbalance in Plasmodium falciparum Transmissible Gametocyte Stages

2018 ◽  
Vol 62 (8) ◽  
Author(s):  
Dina Coertzen ◽  
Janette Reader ◽  
Mariëtte van der Watt ◽  
Sindisiwe H. Nondaba ◽  
Liezl Gibhard ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Malaria Control ◽  
Malaria Parasite ◽  
Redox Homeostasis ◽  
New Drugs ◽  
Content Type ◽  
Artemisinin Derivatives ◽  
Antimalarial Agents ◽  
Redox Partner ◽  
Emergence Of Resistance

ABSTRACT The emergence of resistance toward artemisinin combination therapies (ACTs) by the malaria parasite Plasmodium falciparum has the potential to severely compromise malaria control. Therefore, the development of new artemisinins in combination with new drugs that impart activities toward both intraerythrocytic proliferative asexual and transmissible gametocyte stages, in particular, those of resistant parasites, is urgently required. We define artemisinins as oxidant drugs through their ability to oxidize reduced flavin cofactors of flavin disulfide reductases critical for maintaining redox homeostasis in the malaria parasite. Here we compare the activities of 10-amino artemisinin derivatives toward the asexual and gametocyte stages of P. falciparum parasites. Of these, artemisone and artemiside inhibited asexual and gametocyte stages, particularly stage V gametocytes, in the low-nanomolar range. Further, treatment of both early and late gametocyte stages with artemisone or artemiside combined with the pro-oxidant redox partner methylene blue displayed notable synergism. These data suggest that modulation of redox homeostasis is likely an important druggable process, particularly in gametocytes, and this finding thereby enhances the prospect of using combinations of oxidant and redox drugs for malaria control.

scholarly journals Discovery of oxybisbenzoylamides as a new class of antimalarial agents

MedChemComm ◽  
2015 ◽  
Vol 6 (6) ◽  
pp. 1173-1177 ◽  
Author(s):  
A. Pancotti ◽  
S. Parapini ◽  
M. Dell'Agli ◽  
L. Gambini ◽  
C. Galli ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
New Class ◽  
Antimalarial Agents ◽  
Dual Inhibitors

A new antimalarial pharmacophore has been obtained starting from previously described dual inhibitors of Plasmodium falciparum.

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