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antimalarials

NOT Open Access | Cell Swelling Induced by the Antimalarial KAE609 (Cipargamin) and Other PfATP4-Associated Antimalarials

May 29, 2018 - 14:52 -- NOT Open Access
Author(s): 
Adelaide S. M. Dennis, Adele M. Lehane, Melanie C. Ridgway, John P. Holleran and Kiaran Kirk
Reference: 
Antimicrob. Agents Chemother. June 2018 vol. 62 no. 6 e00087-18

For an increasing number of antimalarial agents identified in high-throughput phenotypic screens, there is evidence that they target PfATP4, a putative Na+ efflux transporter on the plasma membrane of the human malaria parasite Plasmodium falciparum.

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Implications of current therapeutic restrictions for primaquine and tafenoquine in the radical cure of vivax malaria

May 1, 2018 - 15:56 -- Open Access
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Author(s): 
James Watson, Walter R. J. Taylor, Germana Bancone, Cindy S. Chu, Podjanee Jittamala, Nicholas J. White
Reference: 
PLoS Negl Trop Dis 12(4): e0006440

If tafenoquine is deployed for radical cure, primaquine will still be needed to obtain high population coverage.

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In vitro evaluation of chloroquine-loaded and heparin surface-functionalized solid lipid nanoparticles

April 3, 2018 - 15:13 -- Open Access
Author(s): 
Joseph O. Muga, Jeremiah W. Gathirwa, Matshawandile Tukulula and Walter G. Z. O. Jura
Reference: 
Malaria Journal 2018 17:133, 2 April 2018

These findings suggest that the nanoformulated drugs displayed enhanced anti-malarial activities against chloroquine sensitive (D6) strains of P. falciparum compared to the free CQ standard.

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NOT Open Access | Endoperoxide-8-aminoquinoline hybrids as dual-stage antimalarial agents with enhanced metabolic stability

March 21, 2018 - 14:56 -- NOT Open Access
Author(s): 
Rita Capela, Joana Magalhães, Francisca Lopes, et al.
Reference: 
European Journal of Medicinal Chemistry, Volume 149, 10 April 2018, Pages 69-78

Hybrid compounds may play a critical role in the context of the malaria eradication agenda, which will benefit from therapeutic tools active against the symptomatic erythrocytic stage of Plasmodium infection, and also capable of eliminating liver stage parasites.

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NOT Open Access | Pyrazole-pyrazoline as promising novel antimalarial agents: A mechanistic study

March 21, 2018 - 14:54 -- NOT Open Access
Author(s): 
Gautam Kumar, Omprakash Tanwar, Jitender Kumar, Mymoona Akhter, Supriya Sharma, C.R. Pillai, Md Mumtaz Alam, M.S. Zama
Reference: 
European Journal of Medicinal Chemistry, Volume 149, 10 April 2018, Pages 139-147

A series of pyrazole-pyrazoline substituted with benzenesulfonamide were synthesized and evaluated for their antimalarial activity in vitro and in vivo.

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NOT Open Access | Parasite-Mediated Degradation of Synthetic Ozonide Antimalarials Impacts In Vitro Antimalarial Activity

February 28, 2018 - 14:28 -- NOT Open Access
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Author(s): 
Carlo Giannangelo, Lukas Stingelin, Tuo Yang, Leann Tilley, Susan A. Charman and Darren J. Creek
Reference: 
Antimicrob. Agents Chemother. March 2018 vol. 62 no. 3 e01566-17

The peroxide bond of the artemisinins inspired the development of a class of fully synthetic 1,2,4-trioxolane-based antimalarials, collectively known as the ozonides.

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NOT Open Access | Antimalarial naphthoquinones. Synthesis via click chemistry, in vitro activity, docking to PfDHODH and SAR of lapachol-based compounds

February 10, 2018 - 15:54 -- NOT Open Access
Author(s): 
Geraldo Célio Brandão, Franciele C. Rocha Missias, Lucas Miquéias Arantes, Luciana Ferreira Soares, Kuldeep K. Roy, Robert J. Doerksen, Alaide Braga de Oliveira, Guilherme Rocha Pereira
Reference: 
European Journal of Medicinal Chemistry, Volume 145, 10 February 2018, Pages 191-205

Lapachol is an abundant prenyl naphthoquinone occurring in Brazilian Bignoniaceae that was clinically used, in former times, as an antimalarial drug, despite its moderate effect.

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Community participation during two mass anti-malarial administrations in Cambodia: lessons from a joint workshop

January 29, 2018 - 15:45 -- Open Access
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Author(s): 
Thomas J. Peto, Mark Debackere, Jean-Marie Kindermans, et al.
Reference: 
Malaria Journal 2018 17:53, 27 January 2018

Two mass drug administrations (MDA) against falciparum malaria were conducted in 2015–16, one as operational research in northern Cambodia, and the other as a clinical trial in western Cambodia.

Country: 
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NOT Open Access | Astemizole analogues with reduced hERG inhibition as potent antimalarial compounds

November 30, 2017 - 14:51 -- NOT Open Access
Author(s): 
Junjun Tian, Leen Vandermosten, Steve Peigneur, Lien Moreels, Jef Rozenski, Jan Tytgat, Piet Herdewijn, Philippe E. Van den Steen, Steven De Jonghe
Reference: 
Bioorganic & Medicinal Chemistry, Volume 25, Issue 24, 15 December 2017, Pages 6332-6344

Astemizole is a H1-antagonist endowed with antimalarial activity, but has hERG liabilities.

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Proguanil and cycloguanil are organic cation transporter and multidrug and toxin extrusion substrates

October 30, 2017 - 14:52 -- Open Access
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Author(s): 
Maarten van der Velden, Albert Bilos, Jeroen J. M. W. van den Heuvel, Sanna R. Rijpma, Evelien G. E. Hurkmans, Robert W. Sauerwein, Frans G. M. Russel and Jan B. Koenderink
Reference: 
Malaria Journal 2017 16:422, 23 October 2017

Anti-malarials can reduce OCT1 and OCT2 transport activity in vitro.

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