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antimalarials

NOT Open Access | Plants as antimalarial agents in Sub-Saharan Africa

November 10, 2015 - 05:17 -- NOT Open Access
Author(s): 
Kazhila C. Chinsembu
Reference: 
Acta Tropica Volume 152, December 2015, Pages 32–48

Although the burden of malaria is decreasing, parasite resistance to current antimalarial drugs and resistance to insecticides by vector mosquitoes threaten the prospects of malaria elimination in endemic areas.

NOT Open Access | Synthesis, antimalarial activity and molecular docking of hybrid 4-aminoquinoline-1,3,5-triazine derivatives

September 30, 2015 - 17:25 -- NOT Open Access
Author(s): 
Hans Raj Bhat, Udaya Pratap Singh, Anjali Thakur, Surajit Kumar Ghosh, Kabita Gogoi, Anil Prakash, Ramendra K. Singh
Reference: 
Experimental Parasitology, Volume 157, October 2015, Pages 59–67

A series of novel hybrid 4-aminoquinoline 1,3,5-triazine derivatives was synthesized in a five-steps reaction and evaluated for their in vitro antimalarial activity against chloroquine-sensitive (3D7) and chloroquine-resistant (RKL-2) strains of Plasmodium falciparum.

NOT Open Access | The Oral Antimalarial Drug Tafenoquine Shows Activity against Trypanosoma brucei

September 21, 2015 - 16:55 -- NOT Open Access
Author(s): 
Luis Carvalho, Marta Martínez-García, Ignacio Pérez-Victoria, José Ignacio Manzano, Vanessa Yardley, Francisco Gamarro, and José M. Pérez-Victoria
Reference: 
Antimicrob. Agents Chemother. October 2015 vol. 59 no. 10 6151-6160

The protozoan parasite Trypanosoma brucei causes human African trypanosomiasis, or sleeping sickness, a neglected tropical disease that requires new, safer, and more effective treatments.

Medical Treatment: 

NOT Open Access | Highly potent artemisinin-derived dimers and trimers: Synthesis and evaluation of their antimalarial, antileukemia and antiviral activities

September 3, 2015 - 14:30 -- NOT Open Access
Author(s): 
Christoph Reiter, Tony Fröhlich, Svetlana B. Tsogoeva, et al.
Reference: 
Bioorganic & Medicinal Chemistry, Volume 23, Issue 17, 1 September 2015, Pages 5452–5458

New pharmaceutically active compounds can be obtained by modification of existing drugs to access more effective agents in the wake of drug resistance amongst others.

Medical Treatment: 

NOT Open Access | Bayesian models trained with HTS data for predicting β-haematin inhibition and in vitro antimalarial activity

August 12, 2015 - 14:37 -- NOT Open Access
Author(s): 
Kathryn J. Wicht, Jill M. Combrinck, Peter J. Smith, Timothy J. Egan
Reference: 
Bioorganic & Medicinal Chemistry, Volume 23, Issue 16, 15 August 2015, Pages 5210–5217

A large quantity of high throughput screening (HTS) data for antimalarial activity has become available in recent years.

NOT Open Access | Evaluation of spiropiperidine hydantoins as a novel class of antimalarial agents

August 12, 2015 - 14:33 -- NOT Open Access
Author(s): 
Marvin J. Meyers, Elizabeth J. Anderson, Xiaoping Chen, et al.
Reference: 
Bioorganic & Medicinal Chemistry, Volume 23, Issue 16, 15 August 2015, Pages 5144–5150

Given the rise of parasite resistance to all currently used antimalarial drugs, the identification of novel chemotypes with unique mechanisms of action is of paramount importance.

NOT Open Access | Quinoline-based antimalarial hybrid compounds

August 12, 2015 - 14:27 -- NOT Open Access
Author(s): 
Stéphanie Vandekerckhove, Matthias D’hooghe
Reference: 
Bioorganic & Medicinal Chemistry, Volume 23, Issue 16, 15 August 2015, Pages 5098–5119

Quinoline-containing compounds, such as quinine and chloroquine, have a long-standing history as potent antimalarial agents.

Medical Treatment: 

Evaluation of the Diagnostic Accuracy of CareStart G6PD Deficiency Rapid Diagnostic Test (RDT) in a Malaria Endemic Area in Ghana, Africa

April 27, 2015 - 13:11 -- Open Access
Author(s): 
Dennis Adu-Gyasi, Kwaku Poku Asante, Seth Owusu-Agyei, et al.
Reference: 
PLoS ONE 10(4): e0125796

The outcome of this study suggests that the diagnostic performance of the CareStart G6PD deficiency RDT kit was high and it is acceptable at determining the G6PD deficiency status in a high malaria endemic area in Ghana.

Country: 
Medical Treatment: 

Not Open Access | A combination of new screening assays for prioritization of transmission-blocking antimalarials reveals distinct dynamics of marketed and experimental drugs

April 17, 2015 - 14:53 -- NOT Open Access
Author(s): 
J. M. Bolscher, K. M. J. Koolen, G. J. van Gemert, M. G. van de Vegte-Bolmer, T. Bousema, D. Leroy, R. W. Sauerwein, and K. J. Dechering
Reference: 
J. Antimicrob. Chemother. (2015) 70 (5): 1357-1366.

The development of drugs to reduce malaria transmission is an important part of malaria eradication plans. We set out to develop and validate a combination of new screening assays for prioritization of transmission-blocking molecules.

NOT Open Access | Identification of novel class of falcipain-2 inhibitors as potential antimalarial agents

April 14, 2015 - 18:23 -- NOT Open Access
Author(s): 
Sai Kumar Chakka, Mohammad Kalamuddin, Srividhya Sundararaman, Lianhu Wei, Sourabh Mundra, Radhakrishnan Mahesh, Pawan Malhotra, Asif Mohmmed, Lakshmi P. Kotra
Reference: 
Bioorganic & Medicinal Chemistry, Volume 23, Issue 9, 1 May 2015, Pages 2221–2240

Falcipain-2 is a papain family cysteine protease and an emerging antimalarial drug target.

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