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Activities of 11-azaartemisinin and N-sulfonyl derivatives against asexual and transmissible malaria parasites
(Wiley, 2017)
Dihydroartemisinin (DHA), either used in its own right or as the active drug generated in vivo from the other artemisinins in current clinical use—artemether and artesunate—induces quiescence in ring-stage parasites of ...
Inhibition of metalloproteinase-9 secretion and gene expression by artemisinin derivatives
(Elsevier, 2014)
Malaria remains one of the world's most common infectious diseases, being responsible for more deaths than any other communicable disease except tuberculosis. There is strong evidence that tumour necrosis factor α and ...
The evaluation of metal co-ordinating bis-thiosemicarbazones as potential anti-malarial agents
(Bentham Science, 2019)
Background:
The emergence of resistance to the artemisinins which are the current mainstays for antimalarial chemotheraphy has created an environment where the development of new drugs acting in a mechanistally discrete ...
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 ...
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 ...
Development of pyridyl thiosemicarbazones as highly potent agents for the treatment of malaria after oral administration
(Oxford Univ Press, 2019)
Objectives
Drug resistance exists to all current and investigational antimalarial drug classes. Consequently, we have set out to develop chemically and mechanistically discrete antimalarials. Here we report on the development ...
Absorption of the novel artemisinin derivatives artemisone and artemiside: potential application of Pheroid™ technology
(Elsevier, 2011)
Artemisinins have low aqueous solubility that results in poor and erratic absorption upon oral administration. The poor solubility and erratic absorption usually translate to low bioavailability. Artemisinin-based monotherapy ...
Straightforward conversion of decoquinate into inexpensive tractable new derivatives with significant antimalarial activities
(Elsevier, 2016)
As part of a programme aimed at identifying rational new triple drug combinations for treatment of malaria, tuberculosis and toxoplasmosis, we have selected quinolones as one component, given that selected examples exhibit ...
The case for development of 11-aza-artemisinins for malaria
(Bentham Science, 2015)
The current treatment regimens for uncomplicated malaria comprise an artemisinin in combination with another drug (ACT). However, the recent emergence of resistance to ACTs in South East Asia dramatically emphasizes the ...
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 ...