Browsing by Subject "Artemisinins"
Now showing items 1-8 of 8
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Artemisone and artemiside are potent panreactive antimalarial agents that also synergize redox imbalance in Plasmodium falciparum transmissible gametocyte stages
(American Society for Microbiology, 2018)The emergence of resistance toward artemisinin combination therapies (ACTs) by the malaria parasite Plasmodium falciparum has the potential to severely compromise malaria control. Therefore, the development of new artemisinins ... -
Considerations on the mechanism of action of artemisinin antimalarials. Part 1. The 'carbon radical' and 'heme' hypotheses
(Bentham Science, 2013)The isolation of artemisinin from the traditional medicinal herb qīng hāo (Artemisia annua), its characterization as a peroxide and preparation of the derivatives dihydroartemisinin, artemether and artesunate in the 1970s ... -
Evaluation and optimization of synthetic routes from dihydroartemisinin to the alkylamino-artemisinins artemiside and artemisone: a test of N-glycosylation methodologies on a lipophilic peroxide
(Elsevier, 2018)10-Alkylamino-artemisinins including artemiside and artemisone display enhanced activities against malaria. Earlier, dihydroartemisinin (DHA) TMS ether was converted by trimethylsilyl bromide into the 10-β-bromide that ... -
Facile preparation of N-glycosylated 10-piperazinyl artemisinin derivatives and evaluation of their antimalarial and cytotoxic activities
(MDPI, 2018)According to the precepts that C-10 amino-artemisinins display optimum biological activities for the artemisinin drug class, and that attachment of a sugar enhances specificity of drug delivery, polarity and solubility so ... -
In vitro efficacy of synthesized artemisinin derivatives against Leishmania promastigotes
(Elsevier, 2020)Leishmaniasis is a neglected tropical disease affecting thousands worldwide, especially in developing countries where it co-exists with malaria. Only a handful of drugs are clinically available to treat the disease, but ... -
Preliminary evaluation of artemisinin-cholesterol conjugates as potential drugs for the treatment of intractable forms of malaria and tuberculosis
(Wiley, 2018)To evaluate the feasibility of developing drugs that may be active against both malaria and tuberculosis (TB) by using in part putative cholesterol transporters in the causative pathogens and through enhancement of passive ... -
The preparation of artemisinin-cholesterol conjugates as potential new drugs for treatment of intractable forms of tuberculosis and malaria
(North-West University (South Africa) , Potchefstroom Campus, 2016)Malaria and tuberculosis (TB) are two lethal infectious diseases that continue to plague mankind and claim many lives. These diseases are more prevalent in developing countries especially in Africa and Asia. Malaria alone ... -
Synthesis and in vitro antimalarial activity of esters with truncated artemisinin scaffold
(North-West University (South Africa) , Potchefstroom Campus, 2017)Malaria is an infectious disease caused by Plasmodium parasites, with P. falciparum, responsible for most cases of morbidity and mortality. In 2014, malaria killed 438 000 people, with most deaths occurring in sub-Saharan ...