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antimalarial

Disseminating clinical study results to trial participants in Ethiopia: insights and lessons learned

June 9, 2020 - 16:13 -- Open Access
Author(s): 
Tamiru S. Degaga, Sophie Weston, Kamala Thriemer, et al.
Reference: 
Malaria Journal 2020 19:205, 8 June 2020

International regulatory authorities and funders require that research be disseminated promptly and appropriately to all involved stakeholders. However, following completion of clinical trials participants often either do not receive any feedback or materials provided are not appropriate for the context.

Safety, tolerability, pharmacokinetics, and antimalarial efficacy of a novel Plasmodium falciparum ATP4 inhibitor SJ733: a first-in-human and induced blood-stage malaria phase 1a/b trial

April 13, 2020 - 15:18 -- Open Access
Author(s): 
Gaur AH, McCarthy JS, Guy RK, et al.
Reference: 
Lancet Infect Dis. 2020 Apr 7. pii: S1473-3099(19)30611-5

(+)-SJ000557733 (SJ733) is a novel, orally bioavailable inhibitor of Plasmodium falciparum ATP4. In this first-in-human and induced blood-stage malaria phase 1a/b trial, we investigated the safety, tolerability, pharmacokinetics, and antimalarial activity of SJ733 in humans.

NOT Open Access | A multicomponent reaction to design antimalarial pyridyl-indole derivatives: Synthesis, biological activities and molecular docking

April 7, 2020 - 06:06 -- NOT Open Access
Author(s): 
Elshemy HAH, Zaki MA, Mohamed EI, Khan SI, Lamie PF
Reference: 
Bioorganic Chemistry Volume 97, April 2020, 103673

Using fragment-based design strategy, new pyridyl-indole hybrids 4a–y and indole intermediates 3a–e were synthesized using multicomponent one pot reaction. The synthesized compounds were subjected to screening for antimalarial activity against chloroquine sensitive (D6) and chloroquine resistant (W2) strains of Plasmodium falciparum.

NOT Open Access | Antimalarial Eudesmane Sesquiterpenoids from Dobinea delavayi

April 6, 2020 - 15:26 -- NOT Open Access
Author(s): 
Shen Y, Cui SJ, Chen H, Shen L, Wang M, Dong X, Xiao CJ, Jiang B
Reference: 
J Nat Prod. 2020 Apr 1

Eleven new angeloylated eudesmane sesquiterpenoids, dobinins D–N (2, 3, 5, 6, 8, 9, and 11–15), and four known compounds (1, 4, 7, and 10) were isolated from the roots of Dobinea delavayi. A new oxidation product (8a) was also obtained from dobinin H (8). Their structures were elucidated by spectroscopic data and single-crystal X-ray diffraction analyses.

Preclinical Antimalarial Combination Study of M5717, a Plasmodium falciparum Elongation Factor 2 Inhibitor, and Pyronaridine, a Hemozoin Formation Inhibitor

April 6, 2020 - 13:00 -- Open Access
Author(s): 
Matthias Rottmann, Brian Jonat, Thomas Spangenberg, et al.
Reference: 
Antimicrob. Agents Chemother. March 2020 64:e02181-19

Antimalarial drug resistance in the Plasmodium falciparum parasite poses a constant challenge for drug development. To mitigate this risk, new antimalarial medicines should be developed as fixed-dose combinations. Assessing the pharmacodynamic interactions of potential antimalarial drug combination partners during early phases of development is essential in developing the targeted parasitological and clinical profile of the final drug product.

NOT Open Access | Classification models for predicting the antimalarial activity against Plasmodium falciparum

March 23, 2020 - 14:16 -- NOT Open Access
Author(s): 
Liu Q, Deng J, Liu M
Reference: 
SAR QSAR Environ Res. 2020 Mar 19:1-12

Support vector machine (SVM) and general regression neural network (GRNN) were used to develop classification models for predicting the antimalarial activity against Plasmodium falciparum. Only 15 molecular descriptors were used to build the classification models for the antimalarial activities of 4750 compounds, which were divided into a training set (3887 compounds) and a test set (863 compounds).

NOT Open Access | Effect of drug pressure on promoting the emergence of antimalarial resistant parasites among pregnant women in Ghana

March 19, 2020 - 09:16 -- NOT Open Access
Author(s): 
Tornyigah B, Coppée R, Houze P, Kusi KA, Adu B, Quakyi I, Coleman N, Mama A, Deloron P, Anang AK, Clain J, Tahar R, Ofori MF, Ndam NT
Reference: 
Antimicrob Agents Chemother. 2020 Mar 16. pii: AAC.02029-19

Continuous spread of antimalarial drug resistance is a threat to current chemotherapy efficacy. Therefore, characterizing the genetic diversity of drug resistance markers is needed to follow treatment effectiveness and further update control strategies. Here, we genotyped Plasmodium falciparum resistance gene markers associated with sulfadoxine-pyrimethamine (SP) and artemisinin-based combination therapy (ACT) in isolates from pregnant women in Ghana.

NOT Open Access | Chalcone hybrids as privileged scaffolds in antimalarial drug discovery: A key review

March 19, 2020 - 09:07 -- NOT Open Access
Author(s): 
Qin HL, Zhang ZW, Lekkala R, Alsulami H, Rakesh KP
Reference: 
Eur J Med Chem. 2020 Mar 9; 193:112215

Malaria remains a serious worldwide health danger and massive economic trouble to disease-endemic nations. Presently, 250 million of malarial cases are expected worldwide. The emergence of fighting of the Plasmodium parasite against the first-line antimalarial drugs has fueled research attention in the way of designing new scaffolds as well as strategies to counter the drug resistance.

A New Antimalarial Noreudesmane Sesquiterpenoid from Dobinea delavayi

March 2, 2020 - 15:08 -- Open Access
Author(s): 
Wu XR, Shen Y, Cui SJ, Luo XL, Xiao CJ, Jiang B
Reference: 
Nat Prod Bioprospect. 2020 Feb 24

One previously undescribed angeloylated noreudesmane sesquiterpenoid, dobinin O (1), along with four known eudesmane sesquiterpenoids (2–5) were isolated from the peeled roots of Dobinea delavayi.

NOT Open Access | Combination of zingerone and dihydroartemisinin presented synergistic antimalarial activity against Plasmodium berghei infection in BALB/c mice as in vivo model

March 2, 2020 - 14:07 -- NOT Open Access
Author(s): 
Ounjaijean S, Somsak V
Reference: 
Parasitology International, 20 February 2020, 102088

Malaria is a global health problem leading to the death of 435,000 cases in tropical and sub-tropical zones. Spread and emergence of increasing resistance to the antimalarial drugs are the major challenges in the control of malaria. Therefore, searching for alternative antimalarial drugs is urgently needed, and combination treatment preferred as an approach to address this. This study aimed to evaluate in vivo antimalarial activity of zingerone (ZN), and its combination with dihydroartemisinin (DHA) against Plasmodium berghei infected mice.

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