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antimalarial

Clinical determinants of early parasitological response to ACTs in African patients with uncomplicated falciparum malaria: a literature review and meta-analysis of individual patient data

September 9, 2015 - 15:38 -- Open Access
Author(s): 
WWARN Artemisinin based Combination Therapy (ACT) Africa Baseline Study Group
Reference: 
BMC Medicine 2015, 13:212

This study was designed to establish the baseline values for clearance in patients from Sub-Saharan African countries with uncomplicated malaria treated with artemisinin-based combination therapies (ACTs).

Carboxymefloquine, the major metabolite of the antimalarial drug mefloquine, induces drug-metabolizing enzyme and transporter expression by activation of pregnane X receptor.

September 2, 2015 - 16:36 -- Open Access
Author(s): 
Piedade R, Traub S, Bitter A, Nüssler AK, Gil JP, Schwab M, Burk O
Reference: 
Antimicrob Agents Chemother. 2015 Jan;59(1):96-104

Therefore, this study aimed to elucidate the potential of nonartemisinin antimalarial drugs and drug metabolites to activate PXR. We screened 16 clinically used antimalarial drugs and six major drug metabolites for binding to PXR using the two-hybrid PXR ligand binding domain assembly assay; this identified carboxymefloquine, the major and pharmacologically inactive metabolite of the antimalarial drug mefloquine, as a potential PXR ligand. 

Plasmodium falciparum Thioredoxin Reductase (PfTrxR) and Its Role as a Target for New Antimalarial Discovery

July 6, 2015 - 15:30 -- Open Access
Author(s): 
Sara E. McCarty, Amanda Schellenberger, Douglas C. Goodwin, Ngolui Rene Fuanta, Babu L. Tekwani and Angela I. Calderón
Reference: 
Molecules 2015, 20(6), 11459-11473

This review paper provides an overview of the structure and function of TrxR, discusses similarities and differences between the thioredoxin reductases (TrxRs) of different Plasmodium species and the human forms of the enzyme, gives an overview of modeling Plasmodium infections in animals, and suggests the role of Trx functions in antimalarial drug resistance. 

Plasmodium falciparum Thioredoxin Reductase (PfTrxR) and Its Role as a Target for New Antimalarial Discovery

June 24, 2015 - 06:19 -- Open Access
Author(s): 
Sara E. McCarty , Amanda Schellenberger , Douglas C. Goodwin , Ngolui Rene Fuanta , Babu L. Tekwani and Angela I. Calderón
Reference: 
Molecules 2015, 20(6), 11459-11473

This review paper provides an overview of the structure and function of TrxR, discusses similarities and differences between the thioredoxin reductases (TrxRs) of different Plasmodium species and the human forms of the enzyme, gives an overview of modeling Plasmodium infections in animals, and suggests the role of Trx functions in antimalarial drug resistance.

Persistence of chloroquine-resistant haplotypes of Plasmodium falciparum in children with uncomplicated Malaria in Lagos, Nigeria, four years after change of chloroquine as first-line antimalarial medicine

April 28, 2015 - 16:50 -- Open Access
Author(s): 
Oladosu O Oladipo, Oyibo A Wellington and Colin J Sutherland
Reference: 
Diagnostic Pathology 2015, 10:41

This study determined the prevalence of pfcrt haplotypes and point mutations in pfmdr1 genes four years after the change in antimalarial treatment policy from CQ to the ACTs in Lagos, a commercial city in South-West, Nigeria.

NOT Open Access | Synthesis and antimalarial evaluation of prodrugs of novel fosmidomycin analogues

April 27, 2015 - 13:07 -- NOT Open Access
Author(s): 
Ana Maria Faisca Phillips, Fatima Nogueira, Fernanda Murtinheira, Maria Teresa Barros
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 25, Issue 10, 15 May 2015, Pages 2112–2116

The continuous development of drug resistance by Plasmodium falciparum, the agent responsible for the most severe forms of malaria, creates the need for the development of novel drugs to fight this disease.

Antimalarial resistance: is vivax left behind?

September 23, 2014 - 17:08 -- Open Access
Author(s): 
The Lancet Infectious Diseases, Volume 14, Issue 10, October 2014, Pages 908-909
Reference: 
Frédéric Ariey, Richard E Paul

In addition to containing their high-quality analysis, their Article proposes a set of methods to explore resistance to antimalarial drugs in vivax malaria and highlights a surprising scarcity of data and methods available to work on P vivax.

Global extent of chloroquine-resistant Plasmodium vivax: a systematic review and meta-analysis

September 23, 2014 - 17:02 -- Open Access
Author(s): 
Ric N Price, Lorenz von Seidlein, Neena Valecha, Francois Nosten, J Kevin Baird, Nicholas J White
Reference: 
The Lancet Infectious Diseases, Volume 14, Issue 10, October 2014, Pages 982-991

We determined rates of chloroquine resistance according to P vivax malaria recurrence rates by day 28 whole-blood chloroquine concentrations at the time of recurrence and study enrolment criteria.

In vivo antimalarial activity of the crude leaf extract and solvent fractions of Croton macrostachyus Hocsht. (Euphorbiaceae) against Plasmodium berghei in mice

March 20, 2014 - 17:07 -- Open Access
Author(s): 
Laychiluh Bantie, Solomon Assefa, Tilahun Teklehaimanot and Ephrem Engidawork
Reference: 
BMC Complementary and Alternative Medicine 2014, 14:79

This study therefore aimed at investigating the in vivo antiplasmodial activity of 80% methanol extract and solvent fractions of the leaves of Croton macrostachyus H. in rodent model of malaria.

Not Open Access | 1H-1,2,3-Triazole-tethered isatin-7-chloroquinoline and 3-hydroxy-indole-7-chloroquinoline conjugates: Synthesis and antimalarial evaluation

February 5, 2014 - 02:28 -- NOT Open Access
Author(s): 
Raghu Raj, Jiri Gut, Philip J. Rosenthal, Vipan Kumar
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 24, Issue 3, 1 February 2014, Pages 756-759

A series of 1H-1,2,3-triazole-tethered isatin-7-chloroquinoline and 3-hydroxy-indole-7-chloroquinoline conjugates have been synthesized and evaluated for their antimalarial activity against chloroquine-resistant W2 strain of Plasmodium falciparum.

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