scholarly journals Incorporation of an intramolecular hydrogen bonding motif in the side chain of antimalarial benzimidazoles

MedChemComm ◽  
2019 ◽  
Vol 10 (3) ◽  
pp. 450-455 ◽  
Author(s):  
Henrietta D. Attram ◽  
Sergio Wittlin ◽  
Kelly Chibale
Keyword(s):  
Plasmodium Falciparum ◽  
Hydrogen Bonding ◽  
Malaria Parasite ◽  
Intramolecular Hydrogen Bonding ◽  
Side Chain ◽  
Drug Resistant ◽  
Human Malaria Parasite ◽  
Human Malaria ◽  
Intramolecular Hydrogen

Analogues of a novel class of benzimidazoles with an intramolecular hydrogen bonding motif have been synthesized and evaluated in vitro for their antiplasmodium activity against chloroquine-sensitive (NF54) and multi-drug resistant (K1) strains of the human malaria parasite Plasmodium falciparum.

scholarly journals Synthesis of novel β-lactams and in vitro evaluation against the human malaria parasite Plasmodium falciparum

ARKIVOC ◽  
2016 ◽  
Vol 2016 (3) ◽  
pp. 214-235 ◽  
Author(s):  
Margaret A.L. Blackie ◽  
Tzu-Shean Feng ◽  
Peter J Smith ◽  
Kelly Chibale
Keyword(s):  
Plasmodium Falciparum ◽  
Malaria Parasite ◽  
Human Malaria Parasite ◽  
In Vitro Evaluation ◽  
Human Malaria ◽  
Parasite Plasmodium ◽  
Parasite Plasmodium Falciparum

Targeting the human malaria parasite Plasmodium falciparum: In vitro identification of a new antiplasmodial hit in 4-phenoxy-2-trichloromethylquinazoline series

2011 ◽  
Vol 46 (9) ◽  
pp. 4184-4191 ◽  
Author(s):  
Caroline Castera-Ducros ◽  
Nadine Azas ◽  
Pierre Verhaeghe ◽  
Sébastien Hutter ◽  
Philippe Garrigue ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Malaria Parasite ◽  
Human Malaria Parasite ◽  
Human Malaria ◽  
Parasite Plasmodium ◽  
Parasite Plasmodium Falciparum

scholarly journals Polymorphism of a high molecular weight schizont antigen of the human malaria parasite Plasmodium falciparum.

1985 ◽  
Vol 161 (1) ◽  
pp. 160-180 ◽  
Author(s):  
J S McBride ◽  
C I Newbold ◽  
R Anand
Keyword(s):  
Plasmodium Falciparum ◽  
Malaria Parasite ◽  
Peptide Mapping ◽  
Human Malaria Parasite ◽  
Human Malaria ◽  
Parasite Plasmodium ◽  
Parasite Plasmodium Falciparum ◽  
Immunological Classification ◽  
Specific Antigens

Intraspecies antigenic diversity in the blood stages of the human malaria parasite Plasmodium falciparum was investigated using a collection of murine monoclonal antibodies and clones of the parasite. The results were as follows: (a) The schizont and merozoite stages of the parasite express on their surface clonally restricted antigens detectable by strain-specific antibodies in indirect immunofluorescence tests. (b) These restricted antigens are phenotypically stable characteristics of clones grown in vitro. (c) The molecules carrying the specific antigens were isolated by immunoprecipitation and were found to be parasite proteins ranging in size from Mr 190,000 to 200,000 between clones. (d) Comparative immunoprecipitation and peptide mapping of these molecules showed that each parasite clone expresses a protein that is antigenically and structurally distinct from the equivalent products of several other clones. (e) The different clonal products are, however, immunologically interrelated, since they possess determinants in common with all tested isolates of the parasite. (f) These polymorphic molecules are closely related to a previously described schizont protein of P. falciparum that is posttranslationally cleaved into fragments located on the merozoite surface. These findings show the existence of a family of related polymorphic schizont antigens (PSA) of P. falciparum, whose expression is clonally restricted, and indicate that these proteins have regions of constant and variable antigenicity. We propose that a system of immunological classification of the parasite can be developed based on the polymorphism of these proteins.

scholarly journals In Vitro Activity of Riboflavin against the Human Malaria Parasite Plasmodium falciparum

2000 ◽  
Vol 44 (1) ◽  
pp. 88-96 ◽  
Author(s):  
Thomas Akompong ◽  
Nafisa Ghori ◽  
Kasturi Haldar
Keyword(s):  
Plasmodium Falciparum ◽  
Malaria Parasite ◽  
Antimalarial Activity ◽  
Food Vacuole ◽  
Host Cells ◽  
Asexual Parasite ◽  
Human Malaria Parasite ◽  
Human Malaria ◽  
Average Size

ABSTRACT The human malaria parasite Plasmodium falciparumdigests hemoglobin and polymerizes the released free heme into hemozoin. This activity occurs in an acidic organelle called the food vacuole and is essential for survival of the parasite in erythrocytes. Since acidic conditions are known to enhance the auto-oxidation of hemoglobin, we investigated whether hemoglobin ingested by the parasite was oxidized and whether the oxidation process could be a target for chemotherapy against malaria. We released parasites from their host cells and separately analyzed hemoglobin ingested by the parasites from that remaining in the erythrocytes. Isolated parasites contained elevated amounts (38.5% ± 3.5%) of oxidized hemoglobin (methemoglobin) compared to levels (0.8% ± 0.2%) found in normal, uninfected erythrocytes. Further, treatment of infected cells with the reducing agent riboflavin for 24 h decreased the parasite methemoglobin level by 55%. It also inhibited hemozoin production by 50% and decreased the average size of the food vacuole by 47%. Administration of riboflavin for 48 h resulted in a 65% decrease in food vacuole size and inhibited asexual parasite growth in cultures. High doses of riboflavin are used clinically to treat congenital methemoglobinemia without any adverse side effects. This activity, in conjunction with its impressive antimalarial activity, makes riboflavin attractive as a safe and inexpensive drug for treating malaria caused by P. falciparum.

4-Thiophenoxy-2-trichloromethyquinazolines display in vitro selective antiplasmodial activity against the human malaria parasite Plasmodium falciparum

2011 ◽  
Vol 21 (19) ◽  
pp. 6003-6006 ◽  
Author(s):  
Pierre Verhaeghe ◽  
Aurélien Dumètre ◽  
Caroline Castera-Ducros ◽  
Sébastien Hutter ◽  
Michèle Laget ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Malaria Parasite ◽  
Antiplasmodial Activity ◽  
Human Malaria Parasite ◽  
Human Malaria ◽  
Parasite Plasmodium ◽  
Parasite Plasmodium Falciparum

scholarly journals An Investigation on Anti-malarial Effects of Tehranolide Isolated from Artemisia diffusa Against Human Malaria Parasite, Plasmodium falciparum in vitro

2015 ◽  
Vol 10 (2) ◽  
pp. 73-78 ◽  
Author(s):  
Hossein Nahrevania ◽  
Abdolhossein Rustaiyan ◽  
Zahra Zamani ◽  
Mahboubeh Taherkhani ◽  
Aida Iravani
Keyword(s):  
Plasmodium Falciparum ◽  
Malaria Parasite ◽  
Human Malaria Parasite ◽  
Human Malaria ◽  
Parasite Plasmodium ◽  
Parasite Plasmodium Falciparum
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