Targeting Myeloperoxidase Activity and Neutrophil ROS Production to Modulate Redox Process: Effect of Ellagic Acid and Analogues.

Malaria is an infectious disease caused by a genus parasite that remains the most widespread parasitosis. The spread of clones that are increasingly resistant to antimalarial molecules is a serious public health problem for underdeveloped countries. Therefore, the search for new therapeutic approaches is necessary.

Dimeric polyphenols to pave the way for new antimalarial drugs.

Because of the threat of resistant , new orally active antimalarials are urgently needed. Inspired by the structure of ellagic acid, exhibiting potent and antiplasmodial effects, polyphenolic structures possessing a similar activity-safety profile were synthesized. Indeed, most exhibited a marked effect (IC < 4 μM) on resistant , without any detrimental effects reported during the toxicity assays (hemolysis, cytotoxicity, ).

Towards Arginase Inhibition: Hybrid SAR Protocol for Property Mapping of Chlorinated -arylcinnamamides.

A series of seventeen 4-chlorocinnamanilides and seventeen 3,4-dichlorocinnamanilides were characterized for their antiplasmodial activity. In vitro screening on a chloroquine-sensitive strain of 3D7/MRA-102 highlighted that 23 compounds possessed IC < 30 µM. Typically, 3,4-dichlorocinnamanilides showed a broader range of activity compared to 4-chlorocinnamanilides.

Insights into Antimalarial Activity of -Phenyl-Substituted Cinnamanilides.

Due to the urgent need of innovation in the antimalarial therapeutic arsenal, a series of thirty-seven ring-substituted -arylcinnamanilides prepared by microwave-assisted synthesis were subjected to primary screening against the chloroquine-sensitive strain of 3D7/MRA-102. The lipophilicity of all compounds was experimentally determined as the logarithm of the capacity factor , and these data were subsequently used in the discussion of structure-activity relationships. Among the screened compounds, fourteen derivatives exhibited IC from 0.

Polyhydroxybenzoic acid derivatives as potential new antimalarial agents.

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.

Overview of Natural Antiplasmodials from the Last Decade to Inspire Medicinal Chemistry.

Background: Despite major advances in the fight against this parasitic disease, malaria remained a major cause of concern in 2021. This infection, mainly due to Plasmodium falciparum, causes more than 200 million cases every year and hundreds of thousands deaths in the developing regions, mostly in Africa. The last statistics show an increase in the cases for the third consecutive year; from 211 million in 2015, it has reached 229 million in 2019.

In-vitro and in-vivo antimalarial activity of caffeic acid and some of its derivatives.

Objectives: To explore the in-vitro and in-vivo antimalarial potential of caffeic acid and derivatives.

Methods: Two common phenolic acids (caffeic acid and chlorogenic acid) were evaluated for in-vitro and in-vivo antiplasmodial activity in comparison with some semi-synthetic derivatives that were synthesized. An in-vitro assay based on plasmodial lactate dehydrogenase activity, and the classical in-vivo 5-day suppressive test from Peters on an artemisinin-resistant Plasmodium berghei strain was used.