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antimalarial agents

Not Open Access | In-Silico Design, Chemical Synthesis and Biological Screening of Novel 4-(1H)-Pyridone-based Antimalarial Agents

December 7, 2021 - 21:31 -- NOT Open Access
Audu O, Stander A, Ajani O, Egieyeh S, October N
Chem Biol Drug Des. 2021 Nov 30

Identifying novel lead compounds in drug discovery has been challenging because of the rapid rise of drug resistance to the existing chemotherapeutics and a lack of understanding of complex metabolic pathways in the parasite. Integrating computational and experimental approaches has shown to be of great worth in identifying and developing novel promising pharmacophore hybrids.

Not Open Access | Polyhydroxybenzoic acid derivatives as potential new antimalarial agents

August 10, 2021 - 18:07 -- NOT Open Access
Degotte G, Pirotte B, Frédérich M, Francotte P
Arch Pharm (Weinheim). 2021 Aug 4:e2100190

With more than 200 million cases and 400,000 related deaths, malaria remains one of the deadliest infectious diseases of 2021. Unfortunately, despite the availability of efficient treatments, we have observed an increase in people infected with malaria since 2015 (from 211 million in 2015 to 229 million in 2019). This trend could partially be due to the development of resistance to all the current drugs.

Recent Advances in the Biological Investigation of Organometallic Platinum-Group Metal (Ir, Ru, Rh, Os, Pd, Pt) Complexes as Antimalarial Agents

November 18, 2020 - 12:07 -- Open Access
Mbaba M, Golding TM, Smith GS
Molecules. 2020 Nov 12;25(22):E5276

In the face of the recent pandemic and emergence of infectious diseases of viral origin, research on parasitic diseases such as malaria continues to remain critical and innovative methods are required to target the rising widespread resistance that renders conventional therapies unusable. The prolific use of auxiliary metallo-fragments has augmented the search for novel drug regimens in an attempt to combat rising resistance.

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.


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