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antimalarial drug

Drug-Resistant Malaria Detected in Africa Will Require Monitoring

June 16, 2021 - 15:19 -- Open Access
Kuehn BM
JAMA. 2021 Jun 15;325(23):2335

Evidence in Africa that the malaria parasite Plasmodium falciparum has developed genetic variants that confer partial resistance to the antimalarial drug artemisinin is a warning of potential treatment failure on the horizon, a drug-resistance monitoring study suggested.

The high risk of malarial recurrence in patients with Plasmodium-mixed infection after treatment with antimalarial drugs: a systematic review and meta-analysis

May 26, 2021 - 14:40 -- Open Access
Mahittikorn A, Masangkay FR, Kotepui KU, Milanez GJ, Kotepui M
Parasit Vectors. 2021 May 25;14(1):280

Malaria mixed infections are often unrecognized by microscopists in the hospitals, and a delay or failure to treat Plasmodium-mixed infection may lead to aggravated morbidity and increased mortality. The present study aimed to quantify the pooled proportion and risk of malarial recurrences after the treatment of Plasmodium-mixed infection. The results of the study may provide benefits in the management of Plasmodium-mixed infection in co-endemic regions.

NOT Open Access | Plasmodium malariae and Plasmodium falciparum comparative susceptibility to antimalarial drugs in Mali

May 26, 2021 - 09:43 -- NOT Open Access
Dembele L, Aniweh Y, Djimde AA, et al.
J Antimicrob Chemother. 2021 May 22:dkab133

To evaluate Plasmodium malariae susceptibility to current and lead candidate antimalarial drugs.

Methodological approaches for analysing data from therapeutic efficacy studies

May 26, 2021 - 09:16 -- Open Access
Solange Whegang Youdom and Leonardo K. Basco
Malaria Journal 2021 20:228, 21 May 2021

Several anti-malarial drugs have been evaluated in randomized clinical trials to treat acute uncomplicated Plasmodium falciparum malaria. The outcome of anti-malarial drug efficacy studies is classified into one of four possible outcomes defined by the World Health Organization: adequate clinical and parasitological response, late parasitological failure, late clinical failure, early treatment failure.

NOT Open Access | Heme Detoxification in the Malaria Parasite: A Target for Antimalarial Drug Development

May 19, 2021 - 13:36 -- NOT Open Access
de Villiers KA, Egan TJ
Acc Chem Res. 2021 May 13

Over the last century, malaria deaths have decreased by more than 85%. Nonetheless, there were 405 000 deaths in 2018, mostly resulting from Plasmodium falciparum infection. In the 21st century, much of the advance has arisen from the deployment of insecticide-treated bed nets and artemisinin combination therapy. However, over the past few decades parasites with a delayed artemisinin clearance phenotype have appeared in Southeast Asia, threatening further gains. The effort to find new drugs is thus urgent. A prominent process in blood stage malaria parasites, which we contend remains a viable drug target, is hemozoin formation. This crystalline material consisting of heme can be readily seen when parasites are viewed microscopically.

NOT Open Access | An integrated virtual screening and drug repurposing strategy for the discovery of new antimalarial drugs against Plasmodium falciparum phosphatidylinositol 3-kinase

May 18, 2021 - 13:32 -- NOT Open Access
Verma K, Lahariya AK, Dubey S, Verma AK, Das A, Schneider KA, Bharti PK
J Cell Biochem. 2021 May 17

The emergence and spread of drug resistance in Plasmodium falciparum, the parasite causing the most severe form of human malaria, is a major threat to malaria control and elimination programs around the globe. With P. falciparum having evolved widespread resistance against a number of previously widely used drugs, currently, artemisinin (ART) and its derivatives are the cornerstones of first-line treatments of uncomplicated malaria. However, growing incidences of ART failure reflect the spread of ART-resistant P. falciparum strains.

NOT Open Access | Review of the mechanism underlying mefloquine-induced neurotoxicity

April 29, 2021 - 07:14 -- NOT Open Access
Martins AC, Paoliello MMB, Docea AO, Santamaria A, Tinkov AA, Skalny AV, Aschner M
Crit Rev Toxicol. 2021 Apr 27:1-8

Mefloquine, a potent blood schizontocide, is effective against drug-resistant Plasmodium falciparum. This property, along with its unique pharmacokinetic profile, makes mefloquine a widely prescribed antimalarial drug. However, several epidemiological studies have raised concerns on the safety of mefloquine as prophylaxis for malaria. Well-documented side-effects of mefloquine include abnormal dreams, insomnia, anxiety, and depressed mood, as well as nausea and dizziness (the last two most frequent effects).

NOT Open Access | Design, synthesis and biological evaluation of mono- and bisquinoline methanamine derivatives as potential antiplasmodial agents

April 20, 2021 - 15:27 -- NOT Open Access
Bokosi FRB, Beteck RM, Mbaba M, Mtshare TE, Laming D, Hoppe HC, Khanye SD
Bioorg Med Chem Lett. 2021 Apr 15;38:127855

Several classes of antimalarial drugs are currently available, although issues of toxicity and the emergence of drug resistant malaria parasites have reduced their overall therapeutic efficiency. Quinoline based antiplasmodial drugs have unequivocally been long-established and continue to inspire the design of new antimalarial agents. Herein, a series of mono- and bisquinoline methanamine derivatives were synthesised through sequential steps; Vilsmeier-Haack, reductive amination, and nucleophilic substitution, and obtained in low to excellent yields.

NOT Open Access | Plasmodium falciparum Ferredoxin-NADP(+) Reductase-Catalyzed Redox Cycling of Plasmodione Generates Both Predicted Key Drug Metabolites: Implication for Antimalarial Drug Development

April 20, 2021 - 15:10 -- NOT Open Access
Cichocki BA, Donzel M, Heimsch KC, Lesanavičius M, Feng L, Montagut EJ, Becker K, Aliverti A, Elhabiri M, Čėnas N, Davioud-Charvet E
ACS Infect Dis. 2021 Apr 15

Plasmodione (PD) is a potent antimalarial redox-active 3-benzyl-menadione acting at low nanomolar range concentrations on different malaria parasite stages. The specific bioactivation of PD was proposed to occur via a cascade of redox reactions starting from one-electron reduction and then benzylic oxidation, leading to the generation of several key metabolites including corresponding benzylic alcohol (PD-bzol, for PD benzhydrol) and 3-benzoylmenadione (PDO, for PD oxide).

NOT Open Access | Antimalarial drug resistance markers in human immunodeficiency virus (HIV)-positive and HIV-negative adults with asymptomatic malaria infections in Port Harcourt, Nigeria

April 7, 2021 - 12:16 -- NOT Open Access
Chijioke-Nwauche I, Oguike MC, Nwauche CA, Beshir KB, Sutherland CJ
Trans R Soc Trop Med Hyg. 2021 Apr 6:trab061

In Nigeria, indiscriminate use of antimalarial drugs may contribute to the threat of drug resistance, but this has not been evaluated among people living with human immunodeficiency virus (HIV).


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