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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 ...
Corrigendum to ‘In vitro activity of artemisone and artemisinin derivatives against extracellular and intracellular Helicobacter pylori’ [International Journal of Antimicrobial Agents 48/1 (2016) 101–105]
(Elsevier, 2018)
The authors regret that there was an error in the Table 1: The Metronidazole MIC value for the strain E17 should be 2 microg/ml. This is now corrected online.
The authors would like to apologise for any inconvenience caused.
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 ...
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 ...
Absorptive and secretory transport of selected artemisinin derivatives across Caco-2 cell monolayers
(Bentham Science, 2018)
Background: Malaria continues to be a major health concern and affects more than 200 million people a year. Drugs currently used for treatment of malaria are increasingly rendered ineffectual by the ongoing emergence of ...
Accessible and distinct decoquinate derivatives active against Mycobacterium tuberculosis and apicomplexan parasites
(Nature, 2018)
The quinolone decoquinate is coadministered with feed for treatment of parasites which cause coccidiosis in poultry. However, from a drug-development perspective, the biological activity is often not adequately exploited ...
Synthesis, antimalarial activities and cytotoxicities of amino-artemisinin-1,2-disubstituted ferrocene hybrids
(Elsevier, 2018)
Artemisinin-ferrocene conjugates incorporating a 1,2-disubstituted ferrocene analogous to that embedded in ferroquine but attached via a piperazine linker to C10 of the artemisinin were prepared from the piperazine artemisinin ...
Cocrystals of the antimalarial drug 11-azaartemisinin with three alkenoic acids of 1:1 or 2:1 stoichiometry
(IUCr, 2018)
The stoichiometry, X-ray structures and stability of four pharmaceutical cocrystals previously identified from liquid-assisted grinding (LAG) of 11-azaartemisinin (11-Aza; systematic name: 1,5,9-trimethyl-14,15,16-triox ...
Synthesis, in vitro antimalarial activities and cytotoxicities of amino-artemisinin-ferrocene derivatives
(Elsevier, 2018)
Novel derivatives bearing a ferrocene attached via a piperazine linker to C-10 of the artemisinin nucleus were prepared from dihydroartemisinin and screened against chloroquine (CQ) sensitive NF54 and CQ resistant K1 and ...
Formulation of natural oil nano-emulsions for the topical delivery of clofazimine, artemisone and decoquinate
(Springer, 2018)
Purpose
The aim of this study was to formulate nano-emulsions comprising natural oils and the active pharmaceutical ingredients (APIs) clofazimine (CLF), artemisone (ATM) and decoquinate (DQ) in order to determine ...