New medicines to improve control and contribute to the eradication of malaria

TNC Wells, PL Alonso, WE Gutteridge - Nature reviews Drug discovery, 2009 - nature.com
Despite being one of the most prevalent tropical diseases, for many years malaria was not a
commercial priority for the pharmaceutical industry. However, in response to the emergence …

Geminal diheteroatomic motifs: some applications of acetals, ketals, and their sulfur and nitrogen homologues in medicinal chemistry and drug design

YJ Wu, NA Meanwell - Journal of Medicinal Chemistry, 2021 - ACS Publications
Acetals and ketals and their nitrogen and sulfur homologues are often considered to be
unconventional and potentially problematic scaffolding elements or pharmacophores for the …

The state of the art in anti-malarial drug discovery and development

J N. Burrows, K Chibale… - Current topics in medicinal …, 2011 - benthamdirect.com
Malaria is one of the most prevalent and devastating infectious diseases of our time. Yet,
unfortunately, apart from artemisinin combination therapies there are relatively few effective …

Iron and heme metabolism in Plasmodium falciparum and the mechanism of action of artemisinins

N Klonis, DJ Creek, L Tilley - Current opinion in microbiology, 2013 - Elsevier
Highlights•Artemisinin is a pro-drug that is activated by heme or iron.•Hemoglobin
degradation generates an artemisinin activator.•Parasite killing requires exposure to an …

[PDF][PDF] Identification of a 1, 2, 4, 5-tetraoxane antimalarial drug-development candidate (RKA 182) with superior properties to the semisynthetic artemisinins

PM O'Neill, RK Amewu, GL Nixon… - Angewandte Chemie …, 2010 - academia.edu
Artemisinin (1) is an extract of the Chinese wormwood Artemisia annua and has been used
since ancient times to treat malaria.[1] Today, semisynthetic derivatives artesunate (2) and …

Antimalarial peroxides: advances in drug discovery and design

RD Slack, AM Jacobine, GH Posner - MedChemComm, 2012 - pubs.rsc.org
Cyclic peroxides such as the plant-derived 1, 2, 4-trioxane artemisinin and its derivatives are
short-lived, rapidly-acting antimalarials that are now usually combined with standard long …

[HTML][HTML] Synthesis of five-and six-membered cyclic organic peroxides: Key transformations into peroxide ring-retaining products

AO Terent'ev, DA Borisov, VA Vil… - Beilstein Journal of …, 2014 - beilstein-journals.org
The present review describes the current status of synthetic five and six-membered cyclic
peroxides such as 1, 2-dioxolanes, 1, 2, 4-trioxolanes (ozonides), 1, 2-dioxanes, 1, 2 …

Endoperoxide antimalarials: Development, structural diversity and pharmacodynamic aspects with reference to 1, 2, 4-trioxane-based structural scaffold

M Rudrapal, D Chetia - Drug design, development and therapy, 2016 - Taylor & Francis
Malaria disease continues to be a major health problem worldwide due to the emergence of
multidrug-resistant strains of Plasmodium falciparum. In recent days, artemisinin (ART) …

Exploration of artemisinin derivatives and synthetic peroxides in antimalarial drug discovery research

OPS Patel, RM Beteck, LJ Legoabe - European journal of medicinal …, 2021 - Elsevier
Malaria is a life-threatening infectious disease caused by protozoal parasites belonging to
the genus Plasmodium. It caused an estimated 405,000 deaths and 228 million malaria …

Considerations on the mechanism of action of artemisinin antimalarials: Part 1-The'carbon radical'and'heme'hypotheses

R K. Haynes, KW Cheu, D N'Da… - Infectious Disorders …, 2013 - benthamdirect.com
The isolation of artemisinin from the traditional medicinal herb qīng hāo (Artemisia annua),
its characterization as a peroxide and preparation of the derivatives dihydroartemisinin …