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antimalarials

NOT Open Access | Design, synthesis and antimalarial evaluation of novel thiazole derivatives

August 8, 2016 - 10:06 -- NOT Open Access
Author(s): 
José María Bueno, Miguel Carda, Benigno Crespo, Ana Carmen Cuñat, Cristina de Cozar, María Luisa León, J. Alberto Marco, Nuria Roda, Juan F. Sanz-Cervera
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 26, Issue 16, 15 August 2016, Pages 3938–3944

As part of our medicinal chemistry program’s ongoing search for compounds with antimalarial activity, we prepared a series of thiazole analogs and conducted a SAR study analyzing their in vitro activities against the chloroquine-sensitive Plasmodium falciparum 3D7 strain.

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NOT Open Access | Bistacrine derivatives as new potent antimalarials

July 23, 2016 - 17:59 -- NOT Open Access
Author(s): 
Ines Schmidt, Gabriele Pradel, Ludmilla Sologub, Alexandra Golzmann, Che J. Ngwa, Anna Kucharski, Tanja Schirmeister, Ulrike Holzgrabe
Reference: 
Bioorganic & Medicinal Chemistry, Volume 24, Issue 16, 15 August 2016, Pages 3636–3642

Linking two tacrine molecules results in a tremendous increase of activity against Plasmodia in comparison to the monomer.

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NOT Open Access | Synthesis, antimalarial properties and 2D-QSAR studies of novel triazole-quinine conjugates

July 23, 2016 - 17:57 -- NOT Open Access
Author(s): 
Hassan M. Faidallah, Siva S. Panda, Alan R. Katritzky, et al.
Reference: 
Bioorganic & Medicinal Chemistry, Volume 24, Issue 16, 15 August 2016, Pages 3527–3539

Click chemistry technique led to novel 1,2,3-triazole-quinine conjugates 8a–g, 10a–o, 11a–h and 13 utilizing benzotriazole-mediated synthetic approach with excellent yields.

Prevalence of anti-malarial resistance genes in Dakar, Senegal from 2013 to 2014

July 12, 2016 - 16:56 -- Open Access
Author(s): 
Agathe Boussaroque, Bécaye Fall, Bruno Pradines, et al.
Reference: 
Malaria Journal 2016 15:347, 7 July 2016

Despite a decline in the prevalence of chloroquine resistance due to the official withdrawal of the drug and to the introduction of ACT, the spread of resistance to chloroquine has continued.

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NOT Open Access | Straightforward conversion of decoquinate into inexpensive tractable new derivatives with significant antimalarial activities

June 6, 2016 - 17:50 -- NOT Open Access
Author(s): 
Richard M. Beteck, Dina Coertzen, Frans J. Smit, Lyn-Marie Birkholtz, Richard K. Haynes, David D. N’Da
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 26, Issue 13, 1 July 2016, Pages 3006–3009

As part of a programme aimed at identifying rational new triple drug combinations for treatment of malaria, tuberculosis and toxoplasmosis, we have selected quinolones as one component, given that selected examples exhibit exceptionally good activities against the causative pathogens of the foregoing diseases.

NOT Open Access | A Click Chemistry-Based Proteomic Approach Reveals that 1,2,4-Trioxolane and Artemisinin Antimalarials Share a Common Protein Alkylation Profile

April 21, 2016 - 16:33 -- NOT Open Access
Author(s): 
Hanafy M. Ismail, Victoria E. Barton, Matthew Panchana, Sitthivut Charoensutthivarakul, Giancarlo A. Biagini, Stephen A. Ward, Paul M. O'Neill
Reference: 
Angewandte Chemie

Here we investigate this proposition using novel clickable 1,2,4-trioxolane activity based protein-profiling probes (ABPPs). ABPPs with potent antimalarial activity were able to alkylate protein target(s) within the asexual erythrocytic stage of Plasmodium falciparum (3D7). 

‘Some anti-malarials are too strong for your body, they will harm you.’ Socio-cultural factors influencing pregnant women’s adherence to anti-malarial treatment in rural Gambia

April 11, 2016 - 16:30 -- Open Access
Author(s): 
Fatou Jaiteh, Susan Dierickx, Charlotte Gryseels, Sarah O’Neill, Umberto D’Alessandro, Susana Scott, Julie Balen and Koen Peeters Grietens
Reference: 
Malaria Journal 2016 15:195, 11 April 2016

Improving women’s knowledge of malaria in pregnancy is not sufficient to assure adherence to anti-malarial treatment.

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Assessment of the effectiveness of the CD3+ tool to detect counterfeit and substandard anti-malarials

March 1, 2016 - 17:47 -- Open Access
Author(s): 
JaCinta S. Batson, Daniel K. Bempong, Patrick H. Lukulay, Nicola Ranieri, R. Duane Satzger and Leigh Verbois
Reference: 
Malaria Journal 2016 15:119, 25 February 2016

The study revealed the relative effectiveness of the technologies as quality control tools.

Medical Treatment: 

Synergistic anti-malarial action of cryptolepine and artemisinins

February 18, 2016 - 09:47 -- Open Access
Author(s): 
Arnold D. Forkuo, Charles Ansah, Kwesi M. Boadu, Johnson N. Boampong, Elvis O. Ameyaw, Ben A. Gyan, Andrea T. Arku and Michael F. Ofori
Reference: 
Malaria Journal 2016 15:89, 16 February 2016

The combination of CPE with the artemisinin derivatives were safe in the rodent model and showed a synergistic anti-malarial activity in vivo and in vitro.

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NOT Open Access | The Clinically Tested Gardos Channel Inhibitor Senicapoc Exhibits Antimalarial Activity

January 20, 2016 - 15:09 -- NOT Open Access
Author(s): 
Venée N. Tubman, Pedro Mejia, Boris E. Shmukler, Amy K. Bei, Seth L. Alper, James R. Mitchell, Carlo Brugnara, and Manoj T. Duraisingh
Reference: 
Antimicrob. Agents Chemother. January 2016 vol. 60 no. 1 613-616

Senicapoc, a Gardos channel inhibitor, prevented erythrocyte dehydration in clinical trials of patients with sickle cell disease.

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