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anti-malarial drugs

NOT Open Access | Parasite viability is a superior measure of anti-malarial drug activity in humans

November 3, 2020 - 15:02 -- NOT Open Access
Rebelo M, Pawliw R, Gower J, Webb L, Mitchell H, Pava Z, Watts RE, Davenport MP, McCarthy JS, Khoury DS
J Infect Dis. 2020 Oct 29:jiaa678

Artemisinin derivatives are the leading class of antimalarial drugs due to their rapid onset of action and rapid clearance of circulating parasites. The parasite clearance (PC) half-life measures the rate of loss of parasites from blood after treatment, and this is currently used to assess antimalarial activity of novel agents and to monitor resistance. However, a number of recent studies have challenged the use of PC to measure drug activity, arguing that many circulating parasites may be non-viable.

4-Arylthieno[2,3-b]pyridine-2-carboxamides Are a New Class of Antiplasmodial Agents

July 20, 2020 - 15:02 -- Open Access
Schweda SI, Alder A, Gilberger T, Kunick C
Molecules. 2020 Jul 13; 25(14):E3187

Malaria causes hundreds of thousands of deaths every year, making it one of the most dangerous infectious diseases worldwide. Because the pathogens have developed resistance against most of the established anti-malarial drugs, new antiplasmodial agents are urgently needed. In analogy to similar antiplasmodial ketones, 4-arylthieno[2,3-b]pyridine-2-carboxamides were synthesized by Thorpe-Ziegler reactions.

NOT Open Access | Relaxometric studies of erythrocyte suspensions infected by Plasmodium falciparum: a tool for staging infection and testing anti-malarial drugs

July 1, 2020 - 16:38 -- NOT Open Access
Di Gregorio E, Ferrauto G, Schwarzer E, Gianolio E, Valente E, Ulliers D, Aime S, Skorokhod O
Magn Reson Med. 2020 Jun 30

Malaria is a global health problem with the most malignant form caused by Plasmodium falciparum (P. falciparum) . Parasite maturation in red blood cells (RBCs) is accompanied by changes including the formation of paramagnetic hemozoin (HZ) nanocrystals, and increased metabolism and variation in membrane lipid composition. Herein, MR relaxometry (MRR) was applied to investigate water exchange across RBCs’ membrane and HZ formation in parasitized RBCs.

Ex-vivo Sensitivity of Plasmodium falciparum to Common Anti-malarial Drugs: The Case of Kéniéroba, a Malaria Endemic Village in Mali

June 23, 2020 - 15:26 -- Open Access
Traoré K, Diakité SAS, Diakité M, et al.
Drugs R D. 2020 Jun 18

In 2006, the National Malaria Control Program in Mali recommended artemisinin-based combination therapy as the first-line treatment for uncomplicated malaria. Since the introduction of artemisinin-based combination therapy, few reports are available on the level of resistance of Plasmodium falciparum to the most common anti-malarial drugs in Mali.

Prevalence of mutations in the Plasmodium falciparum chloroquine resistance transporter, PfCRT, and association with ex vivo susceptibility to common anti-malarial drugs against African Plasmodium falciparum isolates

June 8, 2020 - 15:27 -- Open Access
Francis Tsombeng Foguim, Hervé Bogreau, Mathieu Gendrot, Joel Mosnier, Isabelle Fonta, Nicolas Benoit, Rémy Amalvict, Marylin Madamet, Sharon Wein and Bruno Pradines
Malaria Journal 2020 19:201, 5 June 2020

The Plasmodium falciparum chloroquine transporter gene (pfcrt) is known to be involved in chloroquine and amodiaquine resistance, and more particularly the mutations on the loci 72 to 76 localized within the second exon. Additionally, new mutations (T93S, H97Y, C101F, F145I, M343L, C350R and G353V) were recently shown to be associated with in vitro reduced susceptibility to piperaquine in Asian or South American P. falciparum strains. However, very few data are available on the prevalence of these mutations and their effect on parasite susceptibility to anti-malarial drugs, and more particularly piperaquine in Africa.

Triple artemisinin-containing combination anti-malarial treatments should be implemented now to delay the emergence of resistance

October 8, 2019 - 15:16 -- Open Access
Nicholas J. White
Malaria Journal 2019 18:338, 11 October 2019

Resistance threatens all our currently available anti-malarial drugs.

Deployment and utilization of next-generation sequencing of Plasmodium falciparum to guide anti-malarial drug policy decisions in sub-Saharan Africa: opportunities and challenges

September 10, 2019 - 15:29 -- Open Access
Deus S. Ishengoma, Queen Saidi, Carol H. Sibley, Cally Roper and Michael Alifrangis
Malaria Journal 2019 18:267, 3 September 2019

Parasite resistance against anti-malarial drugs is a major threat to the ongoing malaria control and elimination strategies.

Structure–activity relationships in a series of antiplasmodial thieno[2,3-b]pyridines

March 26, 2019 - 15:50 -- Open Access
Andreas Masch, Abed Nasereddin, Conrad Kunick, et al.
Malaria Journal 2019 18:89, 21 March 2019

The attachment of alkylamino side chains leads to the improvement of antiplasmodial activity and aqueous solubility of selective PfGSK-inhibitors belonging to the class of 4-phenylthieno[2,3-b]pyridines.

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Artesunate-amodiaquine versus artemether-lumefantrine for the treatment of acute uncomplicated malaria in Congolese children under 10 years old living in a suburban area: a randomized study

November 4, 2015 - 11:55 -- Open Access
Mathieu Ndounga, Pembe Issamou Mayengue, Francine Ntoumi, et al.
Malaria Journal 2015, 14:423 (29 October 2015)

This first randomized study in Brazzaville confirmed the excellent efficacy of these co-formulated anti-malarial drugs in children.

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