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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 ...
Antimalarial and anticancer activities of artemisinin-quinoline hybrid-dimers and pharmacokinetic properties in mice
(Elsevier, 2012)
Malaria, one of the three most important life-threatening infectious diseases, is recommended to be treated with ACT (artemisinin combination therapy) against which Plasmodium falciparum already displayed resistance. Two ...
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 ...
Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy
(Elsevier, 2012)
Malaria and HIV are among the most important global health problems of our time and together are responsible for approximately 3 million deaths annually. These two diseases overlap in many regions of the world including ...
Synthesis and antimalarial activity of ethylene glycol oligomeric ethers of artemisinin
(Wiley, 2011)
Objectives The aim of this study was to synthesize a series of ethylene glycol ether derivatives of the antimalarial drug artemisinin, determine their values for selected physicochemical properties and evaluate their ...
Synthesis, in vitro antimalarial and cytotoxicity of artemisinin-aminoquinoline hybrids
(Elsevier, 2011)
Dihydroartemisinin (DHA) was coupled to different aminoquinoline moieties forming hybrids 9–14, which were then treated with oxalic acid to form oxalate salts (9a–14a). Compounds 9a, 10a, 12, 12a, and 14a showed comparable ...
Synthesis, antimalarial activity and cytotoxicity of 10-aminoethylether derivatives of artemisinin
(Elsevier, 2012)
In this study, a series of 11 10-aminoethylether derivatives of artemisinin were synthesised and their
antimalarial activity against both the chloroquine sensitive (D10) and resistant (Dd2) strains of Plasmodium
falciparum ...
Synthesis and antimalarial activity of ethylene glycol oligomeric ethers of artemisinin
(Wiley, 2011)
Objectives The aim of this study was to synthesize a series of ethylene glycol ether
derivatives of the antimalarial drug artemisinin, determine their values for selected physicochemical
properties and evaluate their ...
In vitro activity of Pheroid vesicles containing antibiotics against Plasmodium falciparum
(Springer Nature, 2012)
The macrolide antibiotics, erythromycin and azithromycin, have been studied for their potential antimalarial activity, but only modest activity has been demonstrated. In this study, we investigated the enhancement of the ...
Synthesis and in vitro biological activities of ferrocenyl-chalcone amides
(Springer, 2016)
A series of aminoferrocenyl–chalcone amides 11–19 were synthesized through condensation of a carboxylic acid-functionalized chalcone 10 with ferrocenylamines, using 1,1′-carbonyldiimidazole as the coupling agent. The ...