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antimalarials

NOT Open Access | Potent dual inhibitors of Plasmodium falciparum M1 and M17 aminopeptidases through optimization of S1 pocket interactions

February 15, 2016 - 18:21 -- NOT Open Access
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Author(s): 
Nyssa Drinkwater, Natalie B. Vinh, Peter J. Scammells, et al.
Reference: 
European Journal of Medicinal Chemistry, Volume 110, 3 March 2016, Pages 43–64

Malaria remains a global health problem, and though international efforts for treatment and eradication have made some headway, the emergence of drug-resistant parasites threatens this progress.

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Distillation Time as Tool for Improved Antimalarial Activity and Differential Oil Composition of Cumin Seed Oil

December 16, 2015 - 16:01 -- Open Access
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Author(s): 
Valtcho D. Zheljazkov, Archana Gawde, Charles L. Cantrell, Tess Astatkie, Vicki Schlegel
Reference: 
PLoS ONE 10(12): e0144120

A steam distillation extraction kinetics experiment was conducted to estimate essential oil yield, composition, antimalarial, and antioxidant capacity of cumin (Cuminum cyminum L.) seed (fruits).

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Prevention of Malaria Resurgence in Greece through the Association of Mass Drug Administration (MDA) to Immigrants from Malaria-Endemic Regions and Standard Control Measures

November 24, 2015 - 15:30 -- Open Access
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Author(s): 
Maria Tseroni, Agoritsa Baka, Christos Hadjichristodoulou, et al.
Reference: 
PLoS Negl Trop Dis 9(11): e0004215

Greece was declared malaria-free in 1974 after a long antimalarial fight.

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Bilayer Effects of Antimalarial Compounds

November 19, 2015 - 06:34 -- Open Access
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Author(s): 
Nicole B. Ramsey, Olaf S. Andersen
Reference: 
PLoS ONE 10(11): e0142401

Because of the perpetual development of resistance to current therapies for malaria, the Medicines for Malaria Venture developed the Malaria Box to facilitate the drug development process.

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NOT Open Access | Exploring clotrimazole-based pharmacophore: 3D-QSAR studies and synthesis of novel antiplasmodial agents

November 10, 2015 - 12:37 -- NOT Open Access
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Author(s): 
Simone Brogi, Margherita Brindisi, Stefania Butini, et al.
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 25, Issue 22, 15 November 2015, Pages 5412–5418

We report herein the generation and validation of a 3D-QSAR model based on a set of antimalarials previously described by us and characterized by a clotrimazole-based pharmacophore.

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NOT Open Access | Antiproliferative and antiplasmodial compounds from selected Streptomyces species

November 10, 2015 - 05:34 -- NOT Open Access
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Author(s): 
L. Harinantenaina Rakotondraibe, Rado Rasolomampianina, David G.I. Kingston, et al.
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 25, Issue 23, 1 December 2015, Pages 5646–5649

In continuation of our ongoing search for bioactive compounds from microbial extracts, we performed antiproliferative and/or antimalarial assays on extracts of 806 microbial species isolated from Madagascan marine organisms, on 1317 species isolated from Madagascan soil samples and on a Streptomyces species (S.4) from a marine sponge collected from the Florida Keys.

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Hydroxyethylamine Based Phthalimides as New Class of Plasmepsin Hits: Design, Synthesis and Antimalarial Evaluation

November 5, 2015 - 05:18 -- Open Access
Author(s): 
Anil K. Singh, Sumit Rathore, Brijesh Rathi, et al.
Reference: 
PLoS ONE 10(10): e0139347

A novel class of phthalimides functionalized with privileged scaffolds was designed, synthesized and evaluated as potential inhibitors of plasmepsin 2 (Ki: 0.99 ± 0.1 μM for 6u) and plasmepsin 4 (Ki: 3.3 ± 0.3 μM for 6t), enzymes found in the digestive vacuole of the plasmodium parasite and considered as crucial drug targets.

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Reduced deformability of parasitized red blood cells as a biomarker for anti-malarial drug efficacy

November 4, 2015 - 13:51 -- Open Access
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Author(s): 
Xiaoyan Deng, Simon Duffy, Marie-Eve Myrand-Lapierre, Kerryn Matthews, Aline Santoso, Yi-Ling Du, Katherine Ryan, Hongshen Ma
Reference: 
Malaria Journal 2015, 14:428 (31 October 2015)

These results demonstrate that rigidification of iRBCs may be used as a biomarker for anti-malarial drug efficacy, as well as for new drug screening.

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NOT Open Access | Investigating proteasome inhibitors as potential adjunct therapies for experimental cerebral malaria

October 28, 2015 - 06:06 -- NOT Open Access
Author(s): 
S. W. Howland, G. X. P. Ng, S. K. Chia and L. Rénia
Reference: 
Parasite Immunology, Volume 37, Issue 11, pages 599–604, November 2015

Aside from antimalarials, there is currently no treatment for cerebral malaria, a fulminant neurological complication of P. falciparum infection that is a leading cause of death in African children.

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Inclusion of gametocyte parameters in anti-malarial drug efficacy studies: filling a neglected gap needed for malaria elimination

October 20, 2015 - 09:14 -- Open Access
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Author(s): 
Rashad Abdul-Ghani, Leonardo Basco, John Beier, Mohammed Mahdy
Reference: 
Malaria Journal 2015, 14:413 (19 October 2015)

Standard anti-malarial drug efficacy and drug resistance assessments neglect the gametocyte parameters in their protocols.

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