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antimalarial

Facile Oxidation of Leucomethylene Blue and Dihydroflavins by Artemisinins: Relationship with Flavoenzyme Function and Antimalarial Mechanism of Action

September 16, 2010 - 18:23 -- Ingeborg van Schayk
Author(s): 
Richard K. Haynes Prof. Dr., Wing-Chi Chan, Ho-Ning Wong Dr., Ka-Yan Li, Wai-Keung Wu, Kit-Man Fan, Herman H. Y. Sung Dr., Ian D. Williams Prof. Dr., Davide Prosperi Dr., Sergio Melato Dr., Paolo Coghi Dr., Diego Monti Prof. Dr.
Reference: 
ChemMedChem Volume 5, Issue 8, pages 1282–1299, August 2, 2010

The antimalarial drug methylene blue (MB) affects the redox behaviour of parasite flavin-dependent disulfide reductases such as glutathione reductase (GR) that control oxidative stress in the malaria parasite.

Reverse-benzamidine antimalarial agents: Design, synthesis, and biological evaluation

September 16, 2010 - 13:26 -- Patrick Sampao
Author(s): 
Olivier Berger, Sharon Wein, Jean-Frederic Duckert, Marjorie Maynadier, Siham El Fangour, Roger Escale, Thierry Durand, Henri Vial, Yen Vo-Hoang
Reference: 
Bioorganic & Medicinal Chemistry Letters, Vol 20, Issue 19, 1 Oct 2010, Pg 5815-5817

In the frame of the development of bis-cationic choline analogs, the RSA of bis-N-alkylamidines were studied and a new series of reverse-benzamidine derivatives was designed.

Bis-alkylamine quindolone derivatives as new antimalarial leads

September 15, 2010 - 13:41 -- Patrick Sampao
Author(s): 
João L., Kaamil G., et al.
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 20, Issue 19, 1 Oct 2010, Pg 5634-5637

Quindolone derivatives, designed to target the malaria parasite digestive vacuole and heme detoxification pathway, have been synthesized by reaction with 2-chloro-N,N-diethylethanamine.

Unusual antimalarial meroditerpenes from tropical red macroalgae

September 14, 2010 - 14:12 -- Patrick Sampao
Author(s): 
E. Paige Stout, Jacques Prudhomme, Karine Le Roch, Craig R. Fairchild, Scott G. Franzblau, William Aalbersberg, Mark E. Hay, Julia Kubanek
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 20, Issue 19, 1 October 2010, Pages 5662-5665

Three antimalarial meroditerpenes have been isolated from two Fijian red macroalgae.

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A Comparison of Methods to Detect and Quantify the Markers of Antimalarial Drug Resistance

September 2, 2010 - 15:04 -- Patrick Sampao
Author(s): 
Ian M. Hastings, Christian Nsanzabana, and Tom A. Smith
Reference: 
Am. J. Trop. Med. Hyg., 83(3), 2010, pp. 489-495

Simple counting dramatically reduced sample size and estimate precision, and we show that analysis of unambiguous samples is biased, leaving maximum likelihood or similar statistical inference as the only practical option.

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Open Access | Anti-folate drug resistance in Africa: meta-analysis of reported dihydrofolate reductase (dhfr) and dihydropteroate synthase (dhps) mutant genotype frequencies in African Plasmodium falciparum parasite populations

September 1, 2010 - 08:07 -- Kabogo Ndegwa
Author(s): 
Sridaran S, McClintock SK, Syphard LM, Herman KM, Barnwell JW, Udhayakumar V
Reference: 
Malaria Journal 2010, 9:247 (30 August 2010)

Increasing prevalence of the dhfr triple mutant and dhps double mutant genotypes in Africa are consistent with the loss of efficacy of SP for treatment of clinical malaria in most parts of this continent.

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Open Access | Antimalarial Exposure Delays Plasmodium falciparum Intra-Erythrocytic Cycle and Drives Drug Transporter Genes Expression

August 26, 2010 - 14:37 -- Kabogo Ndegwa
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Author(s): 
Maria Isabel Veiga, Pedro Eduardo Ferreira, Berit Aydin Schmidt, Ulf Ribacke, Anders Björkman, Ales Tichopad, José Pedro Gil
Reference: 
PLoS ONE 5(8): e12408

Both cell cycle delay and induced gene expression represent potentially important mechanisms for parasites to escape the effect of the antimalarial drug.

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Review: The ABCs of multidrug resistance in malaria

August 23, 2010 - 13:31 -- Patrick Sampao
Author(s): 
Jan B. Koenderink, Reginald A. Kavishe, Sanna R. Rijpma, Frans G.M. Russel
Reference: 
Trends in Parasitology, Volume 26, Issue 9, September 2010, Pages 440-446

Here, we give an overview of the PlasmodiumABC family members with reference to their possible role in multidrug resistance.

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Open Access | Editorial Commentary: Risks and Benefits of Targeted Malaria Treatment Based on Rapid Diagnostic Test Results

August 6, 2010 - 12:54 -- Kabogo Ndegwa
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Author(s): 
Anders Björkman and Andreas Mårtensson
Reference: 
Clinical Infectious Diseases 1 September 2010, Vol. 51, No. 5: 512-514

In this issue of Clinical Infectious Diseases, d’Acremont et al [1] importantly address the clinical safety of withholding antimalarial treatment in febrile children who have a negative result for one of the newly developed rapid diagnostic tests (RDTs) for malaria.

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Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution

July 28, 2010 - 07:56 -- Kabogo Ndegwa
Author(s): 
Takuya Miura, Koushi Hidaka, Tsuyoshi Uemura, Keisuke Kashimoto, Yuto Hori, Yuko Kawasaki, Adam J. Ruben, Ernesto Freire, Tooru Kimura, Yoshiaki Kiso
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 20, Issue 16, 15 August 2010, Pages 4836-4839

We attached 2-aminoethylamino groups to allophenylnorstatine-containing plasmepsin (Plm) inhibitors and investigated SAR of the methyl or ethyl substitutions on the amino groups. Unexpectedly, compounds 22 (KNI-10743) and 25 (KNI-10742) exhibited extremely potent Plm II inhibitory activities (Ki <0.1 nM).

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