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antimalarial

Persistent cognitive and motor deficits after successful antimalarial treatment in murine cerebral malaria

December 7, 2010 - 05:59 -- Patrick Sampao
Author(s): 
Minxian Dai, Sandra E. Reznik, David C. Spray, Louis M. Weiss, Herbert B. Tanowitz, Maria Gulinello, Mahalia S. Desruisseaux
Reference: 
Microbes and Infection, Volume 12, Issues 14-15, December 2010, Pages 1198-1207

After cessation of chloroquine, a comprehensive assessment of cognitive and motor function demonstrated persistence of abnormal behavioral outcomes, 10 days after successful eradication of parasites.

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Comparative embryotoxicity of different antimalarial peroxides: In vitro study using the rat whole embryo culture model (WEC)

November 26, 2010 - 13:05 -- Patrick Sampao
Author(s): 
Monica Longo, Sara Zanoncelli, Marco Brughera, Paolo Colombo, Sergio Wittlin, Jonathan L. Vennerstrom, Joerg Moehrle, J. Carl Craft
Reference: 
Reproductive Toxicology, Volume 30, Issue 4, December 2010, Pages 583-590

In an attempt to establish whether and to what extent activity as antimalarials and embryotoxicity can be divorced, IC50s for activity in Plasmodium falciparum strains and the NOELs for RBCs were compared. From this comparison, arterolane showed a better safety margin than artemisinin.

Technology: 

Design, synthesis and in vitro antimalarial evaluation of triazole-linked chalcone and dienone hybrid compounds

November 16, 2010 - 11:33 -- Kabogo Ndegwa
Author(s): 
Eric M. Guantai, Kanyile Ncokazi, Timothy J. Egan, Jiri Gut, Philip J. Rosenthal, Peter J. Smith, Kelly Chibale
Reference: 
Bioorganic & Medicinal Chemistry, Volume 18, Issue 23, 1 December 2010, Pages 8243-8256

A targeted series of chalcone and dienone hybrid compounds containing aminoquinoline and nucleoside templates was synthesized and evaluated for in vitro antimalarial activity. The Cu(I)-catalyzed cycloaddition of azides and terminal alkynes was applied as the hybridization strategy.

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Antimalarial drugs: Speeding to a new lead

November 15, 2010 - 11:36 -- Patrick Sampao
Author(s): 
Man Tsuey Tse
Reference: 
Nature Reviews Drug Discovery 9, 842 (November 2010)

A public–private partnership has identified a promising new antimalarial compound that is potently effective against a range of Plasmodium species — including some that are resistant to currently used agents — and possesses the pharmacokinetic properties needed to become a viable drug.

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Open Access | Oral Presentation: Antimalarial activity of ulein and proof of its action on the Plasmodium falciparum digestive vacuole

November 5, 2010 - 11:47 -- Patrick Sampao
Author(s): 
Alaíde Braga de Oliveira, Maria Fâni Dolabela, Marinete Marins Póvoa, Cid Aimbiré M Santos, Fernando de Pilla Varotti
Reference: 
Malaria Journal 2010, 9(Suppl 2):O9 (20 October 2010)

We have been investigating plants traditionally used in Brazil to treat malaria and fevers.

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Open Access | Oral Presentation: Progress in the development of Reversed Chloroquine molecules as antimalarial therapy

November 5, 2010 - 09:52 -- Patrick Sampao
Author(s): 
Steven J Burgess, Jane Xu-Kelly, Katherine Liebmann, Bornface Gunsaru, Westin Morrill, David H Peyton
Reference: 
Malaria Journal 2010, 9(Suppl 2):O6 (20 October 2010)

Chloroquine (CQ) resistance in P. falciparum is strongly linked to mutations in the gene pfcrt that gives rise to the protein, PfCRT (P. falciparum chloroquine resistance transporter), located in the parasite's digestive vacuole (DV) membrane [1].

Open Access | Oral Presentation: Identification and characterization of novel Plasmodium falciparum cyclophilins and their roles in the antimalarial actions of cyclosporin A and derivatives

November 4, 2010 - 07:38 -- Patrick Sampao
Author(s): 
Alejandro Marin-Menendez, Angus Bell
Reference: 
Malaria Journal 2010, 9(Suppl 2):O3 (20 October 2010)

We are interested in the role (if any) played by cyclophilins in parasite killing by cyclosporins.

Medical Treatment: 

Identification of inhibitors for putative malaria drug targets among novel antimalarial

November 3, 2010 - 12:16 -- Patrick Sampao
Author(s): 
Gregory J., Alberto J., et al
Reference: 
Molecular and Biochemical Parasitology, Volume 175, Issue 1, January 2011, Pages 21-29

We have taken a high-throughput approach toward identifying novel antimalarial chemical inhibitors of prioritized drug targets for Plasmodium falciparum, excluding targets which are inhibited by currently used drugs.

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Synthesis and antimalarial activities of rhenium bioorganometallics based on the 4-aminoquinoline structure

November 3, 2010 - 11:25 -- Kabogo Ndegwa
Author(s): 
Rodrigo Arancibia, Faustine Dubar, Bruno Pradines, Isabelle Forfar, Daniel Dive, A. Hugo Klahn, Christophe Biot
Reference: 
Bioorganic & Medicinal Chemistry Volume 18, Issue 22, 15 November 2010, Pages 8085-8091

A bioorganometallic approach to malaria therapy led to the discovery of ferroquine (FQ, SSR97193). To assess the importance of the electronic properties of the ferrocenyl group, cyclopentadienyltricarbonylrhenium analogues related to FQ, were synthesized.

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3-Alkylthio-1,2,4-triazine dimers with potent antimalarial activity

September 23, 2010 - 09:10 -- Kabogo Ndegwa
Author(s): 
Kung Ban, Sandra Duffy, Yelena Khakham, Vicky M. Avery, Andrew Hughes, Oliver Montagnat, Kasiram Katneni, Eileen Ryan, Jonathan B. Baell
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 20, Issue 20, 15 October 2010, Pages 6024-6029

We report on the discovery of 3-alkylthio-1,2,4-triazine dimers that are potently toxic to Plasmodium falciparum, with single digit nanomolar activity, and up to several thousand-fold lower toxicity to mammalian cells.

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