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 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.

scholarly journals Comparison of Efficacies of Cysteine Protease Inhibitors against Five Strains of Plasmodium falciparum

2001 ◽  
Vol 45 (3) ◽  
pp. 949-951 ◽  
Author(s):  
Ajay Singh ◽  
Philip J. Rosenthal
Keyword(s):  
Plasmodium Falciparum ◽  
Protease Inhibitors ◽  
Cysteine Protease ◽  
Antimalarial Drug ◽  
Drug Target ◽  
Antimalarial Drugs ◽  
Cross Resistance ◽  
Cysteine Protease Inhibitors ◽  
Antimalarial Agents ◽  
Parasite Strains

ABSTRACT Falcipain-2, a cysteine protease and essential hemoglobinase ofPlasmodium falciparum, is a potential antimalarial drug target. We compared the falcipain-2 sequences and sensitivities to cysteine protease inhibitors of five parasite strains that differ markedly in sensitivity to established antimalarial drugs. The sequence of falcipain-2 was highly conserved, and the sensitivities of all of the strains to falcipain-2 inhibitors were very similar. Thus, cross-resistance between cysteine protease inhibitors and other antimalarial agents is not expected in parasites that are now circulating and falcipain-2 remains a promising chemotherapeutic target.

scholarly journals DOCKING STUDIES OF AMINOHYDANTOIN DERIVATIVES AS ANTIMALARIAL AGENTS

2018 ◽  
Vol 8 (5-s) ◽  
pp. 322-326
Author(s):  
Pooja Mali ◽  
Shourya Pratap ◽  
Raghvendra S. Badhauria ◽  
Himanshu Gurjar
Keyword(s):  
Plasmodium Falciparum ◽  
Lactate Dehydrogenase ◽  
Active Site ◽  
Docking Study ◽  
Docking Studies ◽  
Binding Interaction ◽  
Antimalarial Agents ◽  
Rank Score ◽  
Observable Data ◽  
Virtual Platform

Objective: Docking studies of aminohydantoin derivatives as antimalarial agents. A novel derivative of aminohydantoins was selected from the literature. Method: in-silco studies using docking methodology. The compounds were sketched and energy minimized using Chem draw ultra and Chem 3D ultra respectively. Further, the compounds were docked into Plasmodium falciparum transferase inhibitor (3L7) using Molegro Virtual Platform. Twenty eight compounds were docked into the active site of Pf-lactate dehydrogenase cavity and all of them found to have similar binding interactions of a co-crystalized ligand. Result: The compounds were showed good docking score like moldock score and re-rank score. The finding of docking studies shows a typical molecular interaction pattern with lactate dehydrogenase. The binding interaction information derived from these molecules will be useful in future antimalarial agent design. Conclusion: From the docking study, it was observed that ligands bind to the electrostatic, hydrophobic clamp formed by the residues Asp 76(B), Tyr 190(B), Tyr 80(B) and Lys 72(B) which play an important role for Plasmodium falciparum inhibition.   The binding affinity, grid calculation and RMSD percentage lower and upper   parameters were calculated.   Hence, the observable data indicated that, above compounds can serve as good leads for further modification and optimization in the of treatment malaria. Keywords: Molegro, Chemdraw, aminohydantoins and docking, studies as Plasmodium falciparum, 4RAO, moldock score.

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
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