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antimalarial agents

Not Open Access | Novel class of fast acting antimalarial agents: substituted 15-membered azalides

October 22, 2020 - 15:57 -- NOT Open Access
Perić M, Pešić D, Spaventi R, et al.
Br J Pharmacol. 2020 Oct 21

Efficacy of current antimalarial treatments is declining as a result of increasing antimalarial drug resistance so new and potent antimalarial drugs are urgently needed. Azithromycin, a blockbuster azalide antibiotic, was found useful in malaria therapy but its efficacy in humans is low.

Phosphatidylinositol 3-phosphate and Hsp70 protect Plasmodium falciparum from heat-induced cell death

September 29, 2020 - 13:00 -- Open Access
Lu KY, Pasaje CFA, Srivastava T, Loiselle DR, Niles JC, Derbyshire E
Elife. 2020 Sep 25;9:e56773

Phosphatidylinositol 3-phosphate (PI(3)P) levels in Plasmodium falciparum correlate with tolerance to cellular stresses caused by artemisinin and environmental factors. However, PI(3)P function during the Plasmodium stress response was unknown. Here, we used PI3K inhibitors and antimalarial agents to examine the importance of PI(3)P under thermal conditions recapitulating malarial fever.

Natural Products: A Potential Source of Malaria Transmission Blocking Drugs

September 23, 2020 - 09:00 -- Open Access
Moyo P, Mugumbate G, Eloff JN, Louw AI, Maharaj VJ, Birkholtz LM
Pharmaceuticals (Basel). 2020 Sep 17;13(9):E251

The ability to block human-to-mosquito and mosquito-to-human transmission of Plasmodium parasites is fundamental to accomplish the ambitious goal of malaria elimination. The WHO currently recommends only primaquine as a transmission-blocking drug but its use is severely restricted by toxicity in some populations. New, safe and clinically effective transmission-blocking drugs therefore need to be discovered.

NOT Open Access | Discovery of 3-Cinnamamido-N-Substituted Benzamides as Potential Antimalarial Agents

August 19, 2020 - 09:23 -- NOT Open Access
Liu H, Futamura Y, Wu H, Ishiyama A, Zhang T, Shi T, Zheng Q, Iwatsuki M, Ōmura S, Zou H, Osada H
Med Chem. 2020 Aug 17

Malaria is one of the most devastating parasitic diseases, yet the discovery of antimalarial agents remains profoundly challenging. Very few new antimalarials have been developed in the past 50 years, while the emergence of drug-resistance continues to appear.

NOT Open Access | Design, synthesis and biological evaluation of several aromatic substituted chalcones as antimalarial agents

August 10, 2020 - 16:00 -- NOT Open Access
Gopinathan A, Moidu M, Mukundan M, Ellickal Narayanan S, Narayanan H, Adhikari N
Drug Dev Res. 2020 Aug 6. doi: 10.1002/ddr.21727

Malaria is a communicable disease which is caused by protozoan's mainly Plasmodium species (P. falciparum, P. ovale, P. vivax, P. malariae and P. knowlesi). The increasing resistance of Plasmodium to available malarial drugs poses a great responsibility for the researchers in the field of malaria. To overcome this problem of resistance, this study aimed to design and synthesize a new class of antimalarial agent with chalcone as the main moiety.

Natural Phenolic Compounds and Derivatives as Potential Antimalarial Agents

April 27, 2020 - 12:58 -- Open Access
Mamede L, Ledoux A, Jansen O, Frédérich M
Planta Med. 2020 Apr 23

Malaria is a parasitic disease endemic to tropical and subtropical regions responsible for hundreds of millions of clinical cases and hundreds of thousands of deaths yearly. Its agent, the Plasmodium sp., has a highly variable antigenicity, which accounts for the emergence and spread of resistance to all available treatments. In light of this rising problem, scientists have turned to naturally occurring compounds obtained from plants recurrently used in traditional medicine in endemic areas.

3D-QSAR, docking and ADMET properties of aurone analogues as antimalarial agents

April 27, 2020 - 12:49 -- Open Access
Hadni H, Elhallaoui M
Heliyon. 2020 Apr 18;6(4):e03580

The development of multi-resistant strains of plasmodium parasite has become a global problem, therefore, the discovery of new antimalarial agents is the only available solution. In order to improve and propose new compounds with antimalarial activity, the three-dimensional quantitative structure-activity relationship (3D-QSAR) and molecular docking studies were carried on aurone analogues acting as Qo site inhibitors in cytochrome b.

Antimalarial Agents as Therapeutic Tools Against Toxoplasmosis-A Short Bridge between Two Distant Illnesses

April 6, 2020 - 15:32 -- Open Access
Secrieru A, Costa ICC, O'Neill PM, Cristiano MLS
Molecules. 2020 Mar 30;25(7). pii: E1574

Toxoplasmosis is an infectious disease with paramount impact worldwide, affecting many vulnerable populations and representing a significant matter of concern. Current therapies used against toxoplasmosis are based essentially on old chemotypes, which fail in providing a definitive cure for the disease, placing the most sensitive populations at risk for irreversible damage in vital organs, culminating in death in the most serious cases.

Dual Plasmepsin-Targeting Antimalarial Agents Disrupt Multiple Stages of the Malaria Parasite Life Cycle

March 3, 2020 - 14:54 -- Open Access
Favuzza P, de Lera Ruiz M, Cowman AF, et al.
Cell Host & Microbe, 27 February 2020. pii: S1931-3128(20)30113-X

Artemisin combination therapy (ACT) is the main treatment option for malaria, which is caused by the intracellular parasite Plasmodium. However, increased resistance to ACT highlights the importance of finding new drugs. Recently, the aspartic proteases Plasmepsin IX and X (PMIX and PMX) were identified as promising drug targets. In this study, we describe dual inhibitors of PMIX and PMX, including WM382, that block multiple stages of the Plasmodium life cycle.

NOT Open Access | Indolyl-3-ethanone-α-thioethers: A promising new class of non-toxic antimalarial agents

April 11, 2016 - 16:21 -- NOT Open Access
Archibald L. Svogie, Michelle Isaacs, Heinrich C. Hoppe, Setshaba D. Khanye, Clinton G.L. Veale
European Journal of Medicinal Chemistry, Volume 114, 23 May 2016, Pages 79–88

The success of chemotherapeutics in easing the burden of malaria is under continuous threat from ever-evolving parasite resistance, including resistance to artemisinin combination therapies.

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