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Scientific Articles

Synthesis, antimalarial activity and cytotoxicity of 4-aminoquinoline–triazine conjugates

December 22, 2009 - 12:59 -- Patrick Sampao
Author(s): 
Sunny Manohar, Shabana I. Khan, Diwan S. Rawat
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 20, Issue 1, 1 January 2010, Pages 322-325

A series of 4-aminoquinoline–triazine conjugates with different substitution pattern have been synthesized and evaluated for their in vitro antimalarial activity against chloroquine-sensitive and resistant strains of Plasmodium falciparum.

Antiplasmodial activity of piperazine sulfonamides

December 22, 2009 - 12:50 -- Patrick Sampao
Author(s): 
Derek C. Martyn, Joseph F. Cortese, Erin Tyndall, Justin Dick, Ralph Mazitschek, Benito Munoz, Jon Clardy
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 20, Issue 1, 1 January 2010, Pages 218-221

A high-throughput screening program identified two piperazine sulfonamides with activity against Plasmodium falciparum.

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Synthesis and antiplasmodial activity of novel 2,4-diaminopyrimidines

December 22, 2009 - 12:41 -- Patrick Sampao
Author(s): 
Derek C. Martyn, Amarjit Nijjar, Cassandra A. Celatka, Ralph Mazitschek, Joseph F. Cortese, Erin Tyndall, Hanlan Liu, Maria M. Fitzgerald, Thomas J. O’Shea, Sanjay Danthi, Jon Clardy
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 20, Issue 1, 1 January 2010, Pages 228-231

Two sets of diaminopyrimidines, totalling 45 compounds, were synthesized and assayed against Plasmodium falciparum.

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Antimalarial activity of azadipeptide nitriles

December 22, 2009 - 12:36 -- Patrick Sampao
Author(s): 
Reik Löser, Jiri Gut, Philip J. Rosenthal, Maxim Frizler, Michael Gütschow, Katherine T. Andrews
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 20, Issue 1, 1 January 2010, Pages 252-255

These first generation azadipeptide nitriles represent a promising new class of compounds for antimalarial drug development.

Alkyl and dialkylaminoethyl derivatives of 5-amino-2-azabicyclo[3.2.2]nonanes and their antiplasmodial and antitrypanosomal activities

December 22, 2009 - 12:32 -- Patrick Sampao
Author(s): 
Johanna Faist, Werner Seebacher, Marcel Kaiser, Reto Brun, Robert Saf, Robert Weis
Reference: 
European Journal of Medicinal Chemistry, Volume 45, Issue 1, January 2010, Pages 179-185

N-Alkyl and N-(2-dialkylaminoethyl) derivatives of 5-amino-2-azabicyclo-nonanes were prepared and tested in vitro for their activities against the multidrug-resistant K1 strain of Plasmodium falciparum and Trypanosoma brucei rhodesiense (STIB 900).

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Plasmodium Sporozoite Motility Is Modulated by the Turnover of Discrete Adhesion Sites

December 22, 2009 - 12:21 -- Patrick Sampao
Author(s): 
Sylvia Münter, Benedikt Sabass, Christine Selhuber-Unkel, Mikhail Kudryashev, Stephan Hegge, Ulrike Engel, Joachim P. Spatz, Kai Matuschewski, Ulrich S. Schwarz, Friedrich Frischknecht
Reference: 
Cell Host & Microbe, Volume 6, Issue 6, 17 December 2009, Pages 551-562

Here, we show that sporozoite motility is characterized by a continuous sequence of stick-and-slip phases.

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Open Access| Residual Antimalarials in Malaria Patients from Tanzania – Implications on Drug Efficacy Assessment and Spread of Parasite Resistance

December 22, 2009 - 12:06 -- Ingeborg van Schayk
Author(s): 
Hodel EM, Kabanywanyi AM, Malila A, Zanolari B, Mercier T, et al.
Reference: 
PLoS ONE 4(12): e8184

We report the findings from baseline plasma sampling of malaria patients prior to inclusion into an in vivo study in Tanzania and discuss the implications of residual concentrations of antimalarials in this setting.

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Open Access | IgG Autoantibody to Brain Beta Tubulin III Associated with Cytokine Cluster-II Discriminate Cerebral Malaria in Central India

December 22, 2009 - 11:54 -- Ingeborg van Schayk
Author(s): 
Bansal D, Herbert F, Lim P, Deshpande P, Bécavin C, et al.
Reference: 
PLoS ONE 4(12): e8245

We extended our analysis to an Indian population with genetic backgrounds and endemic and environmental status different from Africa to determine if these autoantibodies could be either a biomarker or a risk factor of developing CM.

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Open Access | High Antibody Titer against Apical Membrane Antigen-1 Is Required to Protect against Malaria in the Aotus Model

December 22, 2009 - 11:48 -- Ingeborg van Schayk
Author(s): 
Dutta S, Sullivan JS, Grady KK, Haynes JD, Komisar J, et al.
Reference: 
PLoS ONE 4(12): e8138

A Plasmodium falciparum 3D7 strain Apical Membrane Antigen-1 (AMA1) vaccine, formulated with AS02A adjuvant, slowed parasite growth in a recent Phase 1/2a trial, however sterile protection was not observed. We tested this AS02A, and a Montanide ISA720 (ISA) formulation of 3D7 AMA1 in Aotus monkeys.

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