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antimalarial

Cutting Edge: Attrition of Plasmodium-Specific Memory CD8 T Cells Results in Decreased Protection That Is Rescued by Booster Immunization

March 22, 2011 - 11:32 -- Kabogo Ndegwa
Author(s): 
Nathan W. Schmidt and John T. Harty
Reference: 
The Journal of Immunology April 1, 2011 vol. 186 no. 7 3836-3840

Sterile protection against infection with Plasmodium sporozoites requires high numbers of memory CD8 T cells.

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Novel thiolactone–isatin hybrids as potential antimalarial and antitubercular agents

March 15, 2011 - 08:15 -- Kabogo Ndegwa
Author(s): 
Renate H. Hans, Ian J.F. Wiid, Paul D. van Helden, Baojie Wan, Scott G. Franzblau, Jiri Gut, Philip J. Rosenthal, Kelly Chibale
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 21, Issue 7, 1 April 2011, Pages 2055-2058

The synthesis of a novel series of thiolactone–isatin hybrids led to the discovery of tetracyclic by-products which displayed superior antiplasmodial activity.

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Synthesis and biological evaluation of benzimidazole-5-carbohydrazide derivatives as antimalarial, cytotoxic and antitubercular agents

March 15, 2011 - 07:38 -- Kabogo Ndegwa
Author(s): 
José Camacho, Arthur Barazarte, Neira Gamboa, Juan Rodrigues, Rosario Rojas, Abraham Vaisberg, Robert Gilman, Jaime Charris
Reference: 
Bioorganic & Medicinal Chemistry, Volume 19, Issue 6, 15 March 2011, Pages 2023-2029

A series of N′-substituted-2-(5-nitrofuran or 5-nitrothiophen-2-yl)-3H-benzo[d]imidazole-5-carbohydrazide derivatives were synthesized and investigated for their abilities to inhibit β-hematin formation, hemoglobin hydrolysis and in vivo for their antimalarial efficacy in rodent Plasmodium berghei.

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Co-expression of the Plasmodium falciparum molecular chaperone, PfHsp70, improves the heterologous production of the antimalarial drug target GTP cyclohydrolase I, PfGCHI

March 14, 2011 - 10:01 -- Patrick Sampao
Author(s): 
Linda L. Stephens, Addmore Shonhai, Gregory L. Blatch
Reference: 
Protein Expression and Purification, Volume 77, Issue 2, June 2011, Pages 159-165

This is the first report of a heterologous co-expression system in which a plasmodial chaperone is harnessed for the improved production and purification of a plasmodial target protein.

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An ethnobotanical study of antimalarial plants in Togo Maritime Region

March 14, 2011 - 09:50 -- Patrick Sampao
Author(s): 
K. Koudouvo, D.S. Karou, K. Kokou, K. Essien, K. Aklikokou, I.A. Glitho, J. Simpore, R. Sanogo, C. De Souza, M. Gbeassor
Reference: 
Journal of Ethnopharmacology, Volume 134, Issue 1, 8 March 2011, Pages 183-190

The present study aimed to document the indigenous medicinal plant utilization for the management of malaria and related symptoms in Togo Maritime Region.

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Traditional herbal antimalarial therapy in Kilifi district, Kenya

March 14, 2011 - 09:20 -- Patrick Sampao
Author(s): 
J.W. Gathirwa, G.M. Rukunga, P.G. Mwitari, N.M. Mwikwabe, C.W. Kimani, C.N. Muthaura, D.M. Kiboi, R.M. Nyangacha, S.A. Omar
Reference: 
Journal of Ethnopharmacology, Volume 134, Issue 2, 24 March 2011, Pages 434-442

This study identified plants with low IC50 values, high percent chemo suppression and low cytotoxicity thus potential sources for novel antiplasmodial agents.

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Reactions of Antimalarial Peroxides with Each of Leucomethylene Blue and Dihydroflavins: Flavin Reductase and the Cofactor Model Exemplified

March 9, 2011 - 08:30 -- Kabogo Ndegwa
Author(s): 
Haynes, R. K., Cheu, K.-W., Tang, M. M.-K., Chen, M.-J., Guo, Z.-F., Guo, Z.-H., Coghi, P. and Monti, D
Reference: 
ChemMedChem, Special Issue: Rare & Neglected Diseases, Volume 6, Issue 2, pages 279–291, February 7, 2011

Flavin adenine dinucleotide (FAD) is reduced by NADPH–E. coli flavin reductase (Fre) to FADH2 in aqueous buffer at pH 7.4 under argon.

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Open Access | Stability-indicating HPLC-DAD/UV-ESI/MS impurity profiling of the anti-malarial drug lumefantrine

March 2, 2011 - 09:11 -- Kabogo Ndegwa
Author(s): 
Verbeken M, Suleman S, Baert B, Vangheluwe E, Van Dorpe S, Burvenich C, Duchateau L, Jansen FH, De Spiegeleer B
Reference: 
Malaria Journal 2011, 10:51 (28 February 2011)

From unstressed, stressed and accelerated stability samples of lumefantrine API and FPPs, nine compounds were detected and characterized to be lumefantrine related impurities.

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An automated, polymer-assisted strategy for the preparation of urea and thiourea derivatives of 15-membered azalides as potential antimalarial chemotherapeutics

March 2, 2011 - 08:36 -- Kabogo Ndegwa
Author(s): 
Antun Hutinec, Renata Rupčić, Dinko Žiher, Kirsten S. Smith, Wilbur Milhous, William Ellis, Colin Ohrt, Zrinka Ivezić Schönfeld
Reference: 
Bioorganic & Medicinal Chemistry, Volume 19, Issue 5, 1 March 2011, Pages 1692-1701

A series of 15-membered azalide urea and thiourea derivatives has been synthesized and evaluated for their in vitro antimalarial activity against chloroquine-sensitive (D6), chloroquine/pyremethamine resistant (W2) and multidrug resistant (TM91C235) strains of Plasmodium falciparum.

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Open Access | Ex Vivo Activity of Histone Deacetylase Inhibitors against Multidrug-Resistant Clinical Isolates of Plasmodium falciparum and P. vivax

March 1, 2011 - 06:28 -- Kabogo Ndegwa
Author(s): 
Jutta Marfurt, Ferryanto Chalfein, Pak Prayoga, Frans Wabiser, Enny Kenangalem, Kim A. Piera, David P. Fairlie, Emiliana Tjitra, Nicholas M. Anstey, Kathy T. Andrews, and Ric N. Price
Reference: 
Antimicrobial Agents and Chemotherapy, March 2011, p. 961-966, Vol. 55, No. 3

Histone acetylation plays an important role in regulating gene transcription and silencing in Plasmodium falciparum.

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