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Plasmodium falciparum ATP4 inhibitors to treat malaria: worthy successors to artemisinin

August 3, 2020 - 15:51 -- Open Access
Ashley EA, Phyo AP
Lancet Infect Dis. 2020 Aug; (8):883-885

Progress in controlling malaria has slowed in recent years and the annual death toll remains above 400 000 globally, with most deaths caused by Plasmodium falciparum.

Insights in chloroquine action: perspectives and implications in Malaria and COVID-19

July 21, 2020 - 12:08 -- Open Access
Pillat MM, Krüger A, Guimarães LMF, Lameu C, de Souza EE, Wrenger C, Ulrich H
Cytometry A. 2020 Jul 19

Malaria is a threat to human mankind and kills about half a million people every year. On the other hand, COVID‐19 resulted in several hundred thousand deaths since December 2019 and remains without an efficient and safe treatment. The antimalarials chloroquine (CQ) and its analogue, hydroxychloroquine (HCQ), have been tested for COVID‐19 treatment, and several conflicting evidence has been obtained.

NOT Open Access | Non-Classical Phenyl Bioisosteres as Effective Replacements in a Series of Novel Open Source Antimalarials

July 20, 2020 - 15:37 -- NOT Open Access
Tse E, Houston SD, Todd MH, et al.
J Med Chem. 2020 Jul 17

The replacement of one chemical motif with another that is broadly similar is a common method in medicinal chemistry to modulate the physical and biological properties of a molecule (i.e. bioisosterism). In recent years, bioisosteres such as cubane and bicyclo[1.1.1]pentane (BCP) have been used as highly effective phenyl mimics. Herein we show the successful incorporation of a range of phenyl bioisosteres during the open source optimization of an antimalarial series.

NOT Open Access | Associations between aminoquinoline resistance genotypes and clinical presentations of Plasmodium falciparum infection in Uganda

July 14, 2020 - 15:58 -- NOT Open Access
Cuu G, Asua V, Tukwasibwe S, Nsobya S, Mpimbaza A, Rosenthal PJ
Antimicrob Agents Chemother. 2020 Jul 13:AAC.00721-20

Mutations that mediate resistance of Plasmodium falciparum to aminoquinoline antimalarials are selected by prior drug use and may alter parasite fitness, but associations with clinical presentations are uncertain. We evaluated genotypes in samples from a case control study of determinants of severe malaria in Ugandan children 4 months to 10 years of age. We studied 274 cases with severe malaria matched by age and geography to 275 uncomplicated malaria controls and 179 asymptomatic parasitemic controls.

NOT Open Access | Extracellular Vesicles Derived from Plasmodium-infected and Non-infected Red Blood Cells as Targeted Drug Delivery Vehicles

July 14, 2020 - 15:36 -- NOT Open Access
Borgheti-Cardoso LN, Kooijmans SAA, Fernàndez-Busquets X, et al.
Int J Pharm. 2020 Jul 9:119627

Among several factors behind drug resistance evolution in malaria is the challenge of administering overall doses that are not toxic for the patient but that, locally, are sufficiently high to rapidly kill the parasites. Thus, a crucial antimalarial strategy is the development of drug delivery systems capable of targeting antimalarial compounds to Plasmodium with high specificity.

The Role of Mass Drug Administration of Antimalarials

July 7, 2020 - 12:51 -- Open Access
Alonso PL
Am. J. Trop. Med. Hyg., 00(00), 2020, pp. 1–2

Either intuition or empiricism must have led to the use of antimalarial drugs to both treat and prevent malaria, pre-dating the identification of the malaria parasite and the mode of its transmission. Josep Masdevall in the XVIII century managed epidemics in Spain through the administration of compounds that included the bark of the cinchona tree. In more recent times, mass drug administration (MDA) was the first form of chemoprevention used against malaria in the early 1900s.

System-wide biochemical analysis reveals ozonide antimalarials initially act by disrupting Plasmodium falciparum haemoglobin digestion

June 29, 2020 - 16:29 -- Open Access
Giannangelo C, Siddiqui G, De Paoli A, Anderson BM, Edgington-Mitchell LE, Charman SA, Creek DJ
PLoS Pathog. 2020 Jun 26;16(6):e1008485

Ozonide antimalarials, OZ277 (arterolane) and OZ439 (artefenomel), are synthetic peroxide-based antimalarials with potent activity against the deadliest malaria parasite, Plasmodium falciparum. Here we used a “multi-omics” workflow, in combination with activity-based protein profiling (ABPP), to demonstrate that peroxide antimalarials initially target the haemoglobin (Hb) digestion pathway to kill malaria parasites. Time-dependent metabolomic profiling of ozonide-treated P. falciparum infected red blood cells revealed a rapid depletion of short Hb-derived peptides followed by subsequent alterations in lipid and nucleotide metabolism, while untargeted peptidomics showed accumulation of longer Hb-derived peptides.

NOT Open Access | Oral-maxillofacial adverse events related to antimalarials

June 8, 2020 - 15:00 -- NOT Open Access
Shuai Y, Wang J, Jiang H, Yu Y, Jin L
Oral Dis. 2020 Jun 4

Malaria is a worldwide parasitic disease, which affects millions of lives every year. Various medications are recommended by WHO for prevention and treatment of malaria. However, adverse events caused by antimalarials were frequently reported, some of which were severe and fatal.

NOT Open Access | Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials

May 13, 2020 - 14:01 -- NOT Open Access
Kancharla P, Dodean RA, Kelly JX, et al.
J Med Chem. 2020 May 11

The global impact of malaria remains staggering despite extensive efforts to eradicate the disease. With increasing drug resistance and the absence of a clinically available vaccine, there is an urgent need for novel, affordable, and safe drugs for prevention and treatment of malaria.

Pan-active imidazolopiperazine antimalarials target the Plasmodium falciparum intracellular secretory pathway

April 15, 2020 - 14:19 -- Open Access
LaMonte GM, Rocamora F, Winzeler EA, et al.
Nat Commun. 2020 Apr 14;11(1):1780

A promising new compound class for treating human malaria is the imidazolopiperazines (IZP) class. IZP compounds KAF156 (Ganaplacide) and GNF179 are effective against Plasmodium symptomatic asexual blood-stage infections, and are able to prevent transmission and block infection in animal models.


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