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NOT Open Access | Artificial Intelligence Applied to the Rapid Identification of New Antimalarial Candidates with Dual-Stage Activity

April 14, 2021 - 08:19 -- NOT Open Access
Lima MNN, Borba JVB, Andrade CH, et al.
ChemMedChem. 2021 Apr 8;16(7):1093-1103

Increasing reports of multidrug-resistant malaria parasites urge the discovery of new effective drugs with different chemical scaffolds. Protein kinases play a key role in many cellular processes such as signal transduction and cell division, making them interesting targets in many diseases. Protein kinase 7 (PK7) is an orphan kinase from the Plasmodium genus, essential for the sporogonic cycle of these parasites.

NOT Open Access | Zwitterionic self-assembled nanoparticles as carriers for Plasmodium targeting in malaria oral treatment

January 31, 2021 - 15:53 -- NOT Open Access
Biosca A, Cabanach P, Abdulkarim M, Gumbleton M, Gómez-Canela C, Ramírez M, Bouzón-Arnáiz I, Avalos-Padilla Y, Borros S, Fernàndez-Busquets X
J Control Release. 2021 Jan 23:S0168-3659(21)00037-7

The current decline in antimalarial drug efficacy due to the evolution of resistant Plasmodium strains calls for new strategies capable of improving the bioavailability of antimalarials, especially of those whose lipophilic character imparts them a low solubility in biological fluids. Here we have designed, synthesized and characterized amphiphilic zwitterionic block copolymers forming nanoparticles capable of penetrating the intestinal epithelium that can be used for oral administration. Poly(butyl methacrylate-co-morpholinoethyl sulfobetaine methacrylate) (PBMA-MESBMA)-based nanoparticles exhibited a specific targeting of Plasmodium falciparum-infected vs. parasite-free red blood cells (74.8%/0.8% respectively), which was maintained upon encapsulation of the lipophilic antimalarial drug curcumin (82.6%/0.3%).

Identification and Assessment of Plasmodium berghei Merozoites and Cell Cycle by Flow Cytometry

January 27, 2021 - 15:36 -- Open Access
Li Q, Xie LH, Zhang J, Pybus BS
Mil Med. 2021 Jan 25;186(Supplement_1):108-115

The asexual blood stages of the Plasmodium berghei life cycle including merozoites are attractive targets for transmission blocking vaccines and drugs. Improved understanding of P. berghei life cycle stage growth and development would provide new opportunities to evaluate antimalarial vaccines and drugs.

Electrocardiographic effects of four antimalarials for pregnant women with uncomplicated malaria on the Thailand-Myanmar border: a randomised controlled trial

January 27, 2021 - 10:15 -- Open Access
Saito M, Yotyingaphiram W, Cargill Z, Gilder ME, Min AM, Phyo AP, San TD, Poe H, Chu C, White NJ, Nosten F, McGready R
Antimicrob Agents Chemother. 2021 Jan 25:AAC.02473-20

Quinoline antimalarials cause drug-induced electrocardiograph QT prolongation, a potential risk factor for torsade de pointes. The effects of currently used antimalarials on the electrocardiogram were assessed in pregnant women with malaria. Pregnant women with microscopy-confirmed parasitaemia of any malaria species were enrolled in an open-label randomised controlled trial on the Thailand-Myanmar border in 2010-2016. Patients were randomised to the standard regimen dihydroartemisinin-piperaquine (DP), artesunate-mefloquine (ASMQ), or an extended regimen of artemether-lumefantrine (AL+). Recurrent vivax infections were treated with chloroquine. Standard 12-lead electrocardiograms were assessed on day 0, 4-6 hour following the last dose and day 7.

NOT Open Access | Current Pharmaceutical Aspects of Synthetic Quinoline Derivatives

December 16, 2020 - 12:19 -- NOT Open Access
Tabassum R, Ashfaq M, Oku H
Mini Rev Med Chem. 2020 Dec 14

Quinoline derivatives are considered as broad spectrum pharmacological compounds that exhibit wide range of biological activities. Integration of quinoline moiety can improve its physical and chemical properties and also pharmacological behavior. Due to its wide range of pharmaceutical applications it is very popular compound to design new drugs for treatment of multiple diseases like cancer, dengue fever, malaria, tuberculosis, fungal infections, AIDS, Alzheimer's disease and diabetes.

NOT Open Access | Antimalarial and anti-inflammatory activities of new chloroquine and primaquine hybrids: Targeting the blockade of malaria parasite transmission

December 16, 2020 - 10:03 -- NOT Open Access
Boechat N, Carvalho RCC, Ferreira MLG, Coutinho JP, Sa PM, Seito LN, Rosas EC, Krettli AU, Bastos MM, Pinheiro LCS
Bioorg Med Chem. 2020 Dec 15;28(24):115832

Malaria is a disease that requires new drugs not only to fight Plasmodium but also to reduce symptoms of infection such as fever and inflammation. A series of 21 hybrid compounds were designed from chloroquine (CQ) and primaquine (PQ) linked to the pharmacophoric group present in phenylacetic anti-inflammatory drugs. These compounds were designed to have dual activity: namely, to be capable of killing Plasmodium and still act on the inflammatory process caused by malaria infection.

NOT Open Access | Self-medication Practice with Antimalarials & the Determinants of Malaria Treatment-Seeking Behavior among Post-partum Mothers in a Rural Community in Nigeria

December 8, 2020 - 10:41 -- NOT Open Access
Iribhogbe OI, Odoya EM
Pharmacoepidemiol Drug Saf. 2020 Dec 6

The majority of the population has inappropriate malaria treatment‐seeking behavior and little is known about self‐medication practice with antimalarials among post‐partum mothers.

NOT Open Access | In silico assessment of natural products and approved drugs as potential inhibitory scaffolds targeting aminoacyl-tRNA synthetases from Plasmodium

November 3, 2020 - 14:45 -- NOT Open Access
Doshi K, Pandya N, Datt M
3 Biotech. 2020 Nov;10(11):470

Malaria remains the leading cause of deaths globally, despite significant advancement towards understanding its epidemiology and availability of multiple therapeutic interventions. Poor efficacy of the approved vaccine, and the rapid emergence of antimalarial drug resistance, warrants an urgent need to expedite the process of development of new lead molecules targeting malaria.

NOT Open Access | Intrinsic fluorescence properties of antimalarial pyrido[1,2-a]benzimidazoles facilitate subcellular accumulation and mechanistic studies in the human malaria parasite Plasmodium falciparum

October 21, 2020 - 09:27 -- NOT Open Access
Korkor CM, Garnie LF, Amod L, Egan TJ, Chibale K
Org Biomol Chem. 2020 Oct 20

The intrinsic fluorescence properties of two related pyrido[1,2-a]benzimidazole antimalarial compounds suitable for the cellular imaging of the human malaria parasite Plasmodium falciparum without the need to attach extrinsic fluorophores are described. Although these compounds are structurally related, they have been shown by confocal microscopy to not only accumulate selectively within P. falciparum but to also accumulate differently in the organelles investigated.

Melatonin action in Plasmodium infection: Searching for molecules that modulate the asexual cycle as a strategy to impair the parasite cycle

October 7, 2020 - 16:04 -- Open Access
Pereira PHS, Garcia CRS
J Pineal Res. 2020 Oct 6:e12700

Half of the world's population lives in countries at risk of malaria infection, which results in approximately 450,000 deaths annually. Malaria parasites infect erythrocytes in a coordinated manner, with cycle durations in multiples of 24 hours, which reflects a behavior consistent with the host's circadian cycle. Interference in cycle coordination can help the immune system to naturally fight infection.


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