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antimalarial

Synthesis and antimalarial activity of thioetherhydroxyethylsulfonamides, potential aspartyl protease inhibitors, Part 3

October 26, 2011 - 06:54 -- Kabogo Ndegwa
Author(s): 
Walcimar T. Vellasco Junior, Guilherme P. Guedes, Thatyana R.A. Vasconcelos, Maria G.F. Vaz, Marcus V.N. de Souza, Antoniana U. Krettli, Luisa G. Krettli, Anna Caroline C. Aguiar, Claudia R.B. Gomes, Wilson Cunico
Reference: 
European Journal of Medicinal Chemistry, Volume 46, Issue 11, November 2011, Pages 5688-5693

MalariaWorldA series of novel thioetherhydroxyethylsulfonamide derivatives has been synthesized from the coupling of intermediates 3-amino-4-phenyl-1-thioetherazine-butan-2-oles 6,7 with arenesulfonyl chlorides in good yields.

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4-aminoquinoline analogues and its platinum (II) complexes as antimalarial agents

October 19, 2011 - 14:27 -- Patrick Sampao
Author(s): 
Nicolli Bellotti de Souza, Arturene M.L. Carmo, Clarice Abramo, et al.
Reference: 
Biomedicine & Pharmacotherapy, Volume 65, Issue 4, July 2011, Pages 313-316

MalariaWorldThese compounds were tested in vivo in a murine model and revealed remarkable inhibition of parasite multiplication values, whose majority ranged from 50 to 80%. In addition they were not cytotoxic. Thus, they may be object of further research for new antimalarial agents.

Synthesis and in vitro antimalarial and antitubercular activity of gold(III) complexes containing thiosemicarbazone ligands

September 27, 2011 - 07:27 -- Patrick Sampao
Author(s): 
Setshaba D. Khanye, Baojie Wan, Scott G. Franzblau, Jiri Gut, Philip J. Rosenthal, Gregory S. Smith
Reference: 
Journal of Organometallic Chemistry, Volume 696, Issue 21

Gold(III) thiosemicarbazone complexes derived from [Au(damp-C1,N)Cl2] (2), where damp = dimeth-ylaminoethylphenyl, have been synthesized. The compounds were characterised using various spectroscopic and analytical techniques, including NMR spectroscopy, mass spectrometry, infrared spectroscopy and elemental analysis.

Polymorphisms of Molecular Markers of Antimalarial Drug Resistance and Relationship with Artesunate-Mefloquine Combination Therapy in Patients with Uncomplicated Plasmodium falciparum Malaria in Thailand

September 8, 2011 - 08:02 -- Patrick Sampao
Author(s): 
Poonuch Muhamad, Papichaya Phompradit, Wannapa Sornjai, Thunyaluk Maensathian, Wanna Chaijaroenkul, Ronnatrai Rueangweerayut and Kesara Na-Bangchang
Reference: 
Am J Trop Med Hyg 2011 vol. 85 no. 3 568-572

Analysis of gene mutation and amplification were performed by nested real-time polymerase chain reaction and SYBR Green I real-time polymerase chain reaction, respectively.

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Potent antimalarial 4-pyridones with improved physico-chemical properties

August 24, 2011 - 10:07 -- Kabogo Ndegwa
Author(s): 
José M. Bueno, Pilar Manzano, Domingo Gargallo-Viola, et al.
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 21, Issue 18, 15 September 2011, Pages 5214-5218

Antimalarial 4-pyridones are a novel class of inhibitors of the plasmodial mitochondrial electron transport chain targeting Cytochrome bc1 (complex III).

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Pharmacokinetics and Ex Vivo Antimalarial Activity of Artesunate-Azithromycin in Healthy Volunteers

August 18, 2011 - 14:58 -- Patrick Sampao
Author(s): 
Nguyen Trong Chinh, Nguyen Ngoc Quang, Michael D. Edstein, et al.
Reference: 
Antimicrobial Agents and Chemotherapy, September 2011,p. 4412-4415, Vol. 55, No. 9

In 18 male healthy subjects, artesunate (200 mg)-azithromycin (1,500 mg) daily for 3 days was found to be well tolerated, with only mild gastrointestinal disturbances reported.

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PG12, a Phospholipid Analog with Potent Antimalarial Activity, Inhibits Plasmodium falciparum CTP:Phosphocholine Cytidylyltransferase Activity

August 16, 2011 - 11:41 -- Patrick Sampao
Author(s): 
Patricia González-Bulnes, April M. Bobenchik, Yoann Augagneur, Rachel Cerdan, Henri J. Vial, Amadeu Llebaria and Choukri Ben Mamoun
Reference: 
August 19, 2011 The Journal of Biological Chemistry, 286, 28940-28947.

Metabolic analyses showed that one of these compounds, PG12, specifically blocks phosphatidylcholine biosynthesis from both the CDP-choline and SDPM pathways via inhibition of PfCCT. In vitro studies using recombinant PfCCT showed a dose-dependent inhibition of the enzyme by PG12.

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Open Access | Artemisinin resistance in Plasmodium falciparum is associated with an altered temporal pattern of transcription

August 8, 2011 - 11:55 -- Patrick Sampao
Author(s): 
Mok S, Imwong M, Bozdech Z, et al.
Reference: 
BMC Genomics 2011, 12:391 (3 August 2011)

To identify key features associated with the delayed parasite clearance phenotype, we employed DNA microarrays to profile the physiological gene expression pattern of the resistant isolates.

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6-Oxopurine Phosphoribosyltransferase: A Target for the Development of Antimalarial Drugs

August 2, 2011 - 14:05 -- Patrick Sampao
Author(s): 
de Jersey, John; Holy, Antonin; Hockova, Dana; Naesens, Lieve; T. Keough, Dianne; W. Guddat, Luke
Reference: 
Current Topics in Medicinal Chemistry, Volume 11, Number 16, August 2011 , pp. 2085-2102(18)

The focus of this review is on the identification and characterization of inhibitors of the enzymes from both Pf and Pv as antimalarial drug leads.

In Vivo and In Vitro Antimalarial Activity of 4-Nerolidylcatechol

August 2, 2011 - 11:09 -- Kabogo Ndegwa
Author(s): 
Luiz Francisco Rocha e Silva, Ana Cristina da Silva Pinto, Valter Ferreira de Andrade-Neto, et al.
Reference: 
Phytotherapy Research, Volume 25, Issue 8, pages 1181–1188, August 2011

4-Nerolidylcatechol (4-NC) isolated from Piper peltatum L. (Piperaceae) was evaluated for in vitro antiplasmodial activity against Plasmodium falciparum (cultures of both standard CQR (K1) and CQS (3D7) strains and two Amazonian field isolates) and for in vivo antimalarial activity using the Plasmodium berghei-murine model.

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