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Thousands of chemical starting points for antimalarial lead identification

May 20, 2010 - 08:05 -- Kabogo Ndegwa
Francisco-Javier Gamo, Laura M. Sanz, Jaume Vidal, Cristina de Cozar, Emilio Alvarez, Jose-Luis Lavandera, Dana E. Vanderwall, Darren V. S. Green, Vinod Kumar, Samiul Hasan
Nature 465, 305-310 (20 May 2010)

Chemical structures and associated data are hereby made public to encourage additional drug lead identification efforts and further research into this disease.

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Open Access | Identification of a Mutant PfCRT-Mediated Chloroquine Tolerance Phenotype in Plasmodium falciparum

May 17, 2010 - 09:12 -- Kabogo Ndegwa
Stephanie G. Valderramos, Juan-Carlos Valderramos, Lise Musset, Lisa A. Purcell, Odile Mercereau-Puijalon, Eric Legrand, David A. Fidock
PLoS Pathog 6(5): e1000887.

Mutant forms of the Plasmodium falciparum transporter PfCRT constitute the key determinant of parasite resistance to chloroquine (CQ), the former first-line antimalarial, and are ubiquitous to infections that fail CQ treatment.

Inhibitory effect of ursolic acid derivatives on hydrogen peroxide- and glutathione-mediated degradation of hemin: A possible additional mechanism of action for antimalarial activity

May 6, 2010 - 12:32 -- Kabogo Ndegwa
Catherine Mullié, Alexia Jonet, Alexandra Dassonville-Klimpt, Grace Gosmann, Pascal Sonnet
Experimental Parasitology, Volume 125, Issue 3, July 2010, Pages 202-207

For GSH degradation pathway, grafting of UA structure with a piperazine structure gave the best inhibition, pleading for the implication of this latter moiety in the inhibitory process.

antimalarial research

May 5, 2010 - 05:55 -- Sankarganesh P

Dear friends,
I am PhD research scholar and antimalarial compound search from endophytic streptomyces species of Medicinal plants origin is my main motto.
i really belive these endophytes for novel source against malarial parasite, it indirectly helps to encourage the forestation process, in which it can reduce the global warming.

A Cell-Based High-Throughput Screen Validates the Plasmodial Surface Anion Channel As an Antimalarial Target

April 21, 2010 - 12:01 -- Patrick Sampao
Ajay D. Pillai, Margaret Pain, Tsione Solomon, Abdullah A. B. Bokhari and Sanjay A. Desai Molecular Pharmacology
Molecular Pharmacology

Approximately 70,000 compounds from synthetic and natural product libraries were screened, revealing inhibitors from multiple structural classes including two novel and potent heterocyclic scaffolds.

Development of a New Generation of 4-Aminoquinoline Antimalarial Compounds Using Predictive Pharmacokinetic and Toxicology Models

April 13, 2010 - 14:06 -- Kabogo Ndegwa
Sunetra Ray, Peter B. Madrid, Paul Catz, Susanna E. LeValley, Michael J. Furniss, Linda L. Rausch, R. Kiplin Guy, Joseph L. DeRisi, Lalitha V. Iyer, Carol E. Green and Jon C. Mirsalis
J. Med. Chem. April 5, 2010

ADMET prediction studies were employed to evaluate a library of new molecules based on the 4-aminoquinolone-related structure of CQ. Extensive in vitro screening and in vivo pharmacokinetic studies in mice helped to identify two lead molecules, 18 and 4, with promising in vitro therapeutic efficacy, improved ADMET properties, low risk for drug−drug interactions, and desirable pharmacokinetic profiles.

Open Access | Further Evidence Supporting a Role for Gs Signal Transduction in Severe Malaria Pathogenesis

April 8, 2010 - 12:56 -- Kabogo Ndegwa
Sarah Auburn, Andrew E. Fry, Taane G. Clark, Susana Campino, Mahamadou Diakite, Angela Green, Anna Richardson, Muminatou Jallow, Fatou Sisay-Joof, Margaret Pinder, Malcolm E. Molyneux, Terrie E. Taylor, Kasturi Haldar, Kirk A. Rockett, Dominic P. Kwiatkowski
PLoS ONE 5(4): e10017.

Having previously demonstrated a role for the G-alpha-s gene, GNAS, in severe malaria disease, we sought to identify other important components of the Gs pathway.

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Synthesis and structure–activity relationships of antimalarial 4-oxo-3-carboxyl quinolones

April 7, 2010 - 11:14 -- Kabogo Ndegwa
Yiqun Zhang, W. Armand Guiguemde, Martina Sigal, Fangyi Zhu, Michele C. Connelly, Solomon Nwaka, R. Kiplin Guy
Bioorganic & Medicinal Chemistry, Volume 18, Issue 7, 1 April 2010, Pages 2756-2766

The increasing prevalence of multi-drug-resistant Plasmodium falciparum drives the ongoing need for the development of new antimalarial drugs.

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Open Access | A cell-based high-throughput screen validates the plasmodial surface anion channel as an antimalarial target

February 1, 2010 - 10:48 -- Ingeborg van Schayk
Ajay D. Pillai, Margaret Pain, Tsione Solomon, Abdullah A.B. Bokhari, and Sanjay A Desai
Mol. Pharmacol. published 25 January 2010

A statistically significant correlation between channel inhibition and in vitro parasite killing by a family of compounds provided chemical validation of PSAC as a drug target. 

Synthesis and antimalarial evaluation of 1, 3, 5-trisubstituted pyrazolines

January 14, 2010 - 18:19 -- Kabogo Ndegwa
Badri Narayan Acharyaa, Deepika Saraswata, Mugdha Tiwaria, Asish Kumar Shrivastavaa, Ramarao Ghorpadea, Saroj Bapnab and Mahabir Parshad Kaushika
European Journal of Medicinal Chemistry Volume 45, Issue 2, February 2010, Pages 430-438

A series of 1,3,5-trisubstituted pyrazolines were synthesized and evaluated for in vitro antimalarial efficacy against chloroquine sensitive (MRC-02) as well as chloroquine resistant (RKL9) strains of Plasmodium falciparum.

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