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antimalarials

NOT Open Access | Absence of Association between Polymorphisms in the RING E3 Ubiquitin Protein Ligase Gene and Ex Vivo Susceptibility to Conventional Antimalarial Drugs in Plasmodium falciparum Isolates from Dakar, Senegal

August 1, 2016 - 11:08 -- NOT Open Access
Author(s): 
Mathieu Gendrot, Bécaye Fall, Bruno Pradines, et al.
Reference: 
Antimicrob. Agents Chemother. August 2016 vol. 60 no. 8 5010-5013

The RING E3 ubiquitin protein ligase is crucial for facilitating the transfer of ubiquitin.

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NOT Open Access | Antimalarial Benzoxaboroles Target Plasmodium falciparum Leucyl-tRNA Synthetase

August 1, 2016 - 11:07 -- NOT Open Access
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Author(s): 
Ebere Sonoiki, Andres Palencia, Philip J. Rosenthal, et al.
Reference: 
Antimicrob. Agents Chemother. August 2016 vol. 60 no. 8 4886-4895

There is a need for new antimalarials, ideally with novel mechanisms of action. Benzoxaboroles have been shown to be active against bacteria, fungi, and trypanosomes.

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Molecular Mechanisms for Drug Hypersensitivity Induced by the Malaria Parasite’s Chloroquine Resistance Transporter

August 1, 2016 - 10:58 -- Open Access
Author(s): 
Sashika N. Richards, Megan N. Nash, Eileen S. Baker, Michael W. Webster, Adele M. Lehane, Sarah H. Shafik, Rowena E. Martin
Reference: 
PLoS Pathog 12(7): e1005725

Mutations in the Plasmodium falciparum ‘chloroquine resistance transporter’ (PfCRT) confer resistance to chloroquine (CQ) and related antimalarials by enabling the protein to transport these drugs away from their targets within the parasite’s digestive vacuole (DV).

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OptiMal-PK: an internet-based, user-friendly interface for the mathematical-based design of optimized anti-malarial treatment regimens

July 11, 2016 - 16:11 -- Open Access
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Author(s): 
Ghaith Aljayyoussi, Katherine Kay, Stephen A. Ward and Giancarlo A. Biagini
Reference: 
Malaria Journal 2016 15:344, 7 July 2016

OptiMal-PK is designed to be implemented by medicinal chemists and pharmacologists during the pre-clinical anti-malarial drug development phase to explore the impact of different PK/PD parameters upon the predicted clinical activity of any new compound.

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Combating poor-quality anti-malarial medicines: a call to action

June 1, 2016 - 15:22 -- Open Access
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Author(s): 
Quique Bassat, Marcel Tanner, Philippe J. Guerin, Kirstin Stricker and Kamal Hamed
Reference: 
Malaria Journal 2016 15:302, 1 June 2016

The circulation of poor-quality medicines continues to undermine the fight against many life-threatening diseases.

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NOT Open Access | Exploration of 3-methylisoquinoline-4-carbonitriles as protein kinase A inhibitors of Plasmodium falciparum

May 3, 2016 - 14:48 -- NOT Open Access
Author(s): 
Melissa J. Buskes, Katherine L. Harvey, Boris Prinz, Brendan S. Crabb, Paul R. Gilson, David J.D. Wilson, Belinda M. Abbott
Reference: 
Bioorganic & Medicinal Chemistry, Volume 24, Issue 11, 1 June 2016, Pages 2389–2396

A series of isoquinolines have been evaluated in a homology model of Plasmodium falciparum Protein Kinase A (PfPKA) using molecular dynamics.

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NOT Open Access | Inhibition of Glutathione Biosynthesis Sensitizes Plasmodium berghei to Antifolates

April 27, 2016 - 17:00 -- NOT Open Access
Author(s): 
Warangkhana Songsungthong, Pongpisid Koonyosying, Chairat Uthaipibull, and Sumalee Kamchonwongpaisan
Reference: 
Antimicrob. Agents Chemother. May 2016 vol. 60 no. 5 3057-3064

Glutathione plays a central role in maintaining cellular redox homeostasis, and modulations to this status may affect malaria parasite sensitivity to certain types of antimalarials.

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NOT Open Access | Inhibition of Plasmodium falciparum proliferation in vitro by double-stranded RNA nanoparticle against malaria topoisomerase II

April 7, 2016 - 18:01 -- NOT Open Access
Author(s): 
Pongsopee Attasart, Siriwan Boonma, Panya Sunintaboon, Dolpawan Tanwilai, Jinrapa Pothikasikorn, Wilai Tienrungroj Noonpakdee
Reference: 
Experimental Parasitology, Volume 164, May 2016, Pages 84–90

The need to develop new effective antimalarial agents is urgent due to the rapid emergence of drug resistance to all current drugs by the most virulent human malaria parasite, Plasmodium falciparum.

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NOT Open Access | Design, synthesis and antimalarial screening of some hybrid 4-aminoquinoline-triazine derivatives against pf-DHFR-TS

March 19, 2016 - 18:38 -- NOT Open Access
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Author(s): 
Supriya Sahu, Surajit Kumar Ghosh, Junmoni Kalita, Mayurakhi Dutta, Hans Raj Bhat
Reference: 
Experimental Parasitology, Volume 163, April 2016, Pages 38–45

Existing antifolate antimalarial drugs have shown resistance due to the mutations at some amino acid positions of Plasmodium falciparum DHFR-TS.

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Seeking treatment for uncomplicated malaria: experiences from the Kintampo districts of Ghana

February 23, 2016 - 17:06 -- Open Access
Author(s): 
Lawrence G. Febir, Kwaku Poku Asante, Samuel Afari-Asiedu, Livesy N. Abokyi, Anthony Kwarteng, Bernhards Ogutu, Margaret Gyapong and Seth Owusu-Agyei
Reference: 
Malaria Journal 2016 15:108, 20 February 2016

There is no clear cut trajectory for management of uncomplicated malaria in the study area. Different approaches are adopted when treating malaria.

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