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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
Elshemy HAH, Zaki MA, Mohamed EI, Khan SI, Lamie PF
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
Shen Y, Cui SJ, Chen H, Shen L, Wang M, Dong X, Xiao CJ, Jiang B
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
Matthias Rottmann, Brian Jonat, Thomas Spangenberg, et al.
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
Liu Q, Deng J, Liu M
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
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
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
Qin HL, Zhang ZW, Lekkala R, Alsulami H, Rakesh KP
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
Wu XR, Shen Y, Cui SJ, Luo XL, Xiao CJ, Jiang B
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
Ounjaijean S, Somsak V
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.

Not Open Access | The Antimalarial Natural Product Salinipostin A Identifies Essential α/β Serine Hydrolases Involved in Lipid Metabolism in P. falciparum Parasites

February 24, 2020 - 13:40 -- NOT Open Access
Yoo E, Schulze CJ, Stokes BH, Onguka O, Yeo T, Mok S, Gnädig NF, Zhou Y, Kurita K, Foe IT, Terrell SM, Boucher MJ, Cieplak P, Kumpornsin K, Lee MCS, Linington RG, Long JZ, Uhlemann AC, Weerapana E, Fidock DA, Bogyo M
Cell Chem Biol. 2020 Feb 20;27(2):143-157.e5

Salinipostin A (Sal A) is a potent antiplasmodial marine natural product with an undefined mechanism of action. Using a Sal A-derived activity-based probe, we identify its targets in the Plasmodium falciparum parasite. All of the identified proteins contain α/β serine hydrolase domains and several are essential for parasite growth. One of the essential targets displays a high degree of homology to human monoacylglycerol lipase (MAGL) and is able to process lipid esters including a MAGL acylglyceride substrate.

NOT Open Access | Potential antimalarial activity of Coccinia barteri leaf extract and solvent fractions against Plasmodium berghei infected mice

February 17, 2020 - 12:03 -- NOT Open Access
Orabueze CI, Obi E, Adesegun SA, Coker HA
Journal of Ethnopharmacology, Volume 248, 10 February 2020, 112334

Coccinia barteri (Hook. F.) is traditional used in Southeast of Nigeria in management of fever. This study aimed to evaluate the antimalarial activities of hydro-methanol crude extract and solvent fractions of Coccinia barteri leaf.


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