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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
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 ...
Preliminary evaluation of artemisinin-cholesterol conjugates as potential drugs for the treatment of intractable forms of malaria and tuberculosis
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 ...
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 ...
Facile preparation of N-glycosylated 10-piperazinyl artemisinin derivatives and evaluation of their antimalarial and cytotoxic activities
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 ...