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Now showing items 21-30 of 44
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 ...
Mono-, di- and trisubstituted derivatives of eflornithine: synthesis for in vivo delivery of DL-alpha-difluoromethylornithine in plasma
(Thieme, 2011)
The aim of this study was to synthesize a series of mono-, di- and trisubstituted derivatives of the human African trypanosomiasis drug eflornithine (alpha-difluoromethylornithine, DMFO, CAS 70052-12-9) to determine their ...
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 and in vitro antiplasmodial activity of quinoline-ferrocene esters
(Thieme, 2011)
New 4-aminoquinoline-derived esters containing the redox-active ferrocene group brought in by either ferrocenyformic or 4-ferrocenylbutanoic acids were synthesized and tested in vitro for their antiplasmodial activity. The ...
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 ...
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 and in vitro human skin penetration of oligo- and polymeric ethylene glycol carbonates of zidovudine and stavudine
(Thieme, 2010)
In continuation of studies focusing on the transdermal delivery of antiretroviral (ARV) drugs, the skin permeation ability of synthesized homologous series of both oligomeric and polymeric ethylene glycol (PEG) carbonates ...
Prodrug strategies for enhancing the percutaneous absorption of drugs
(MDPI, 2014)
The transdermal application of drugs has attracted increasing interest over the last
decade or so, due to the advantages it offers, compared to other delivery methods. The
development of an efficient means of transdermal ...
Recent progress in the development of anti-malarial quinolones
(BioMed Central, 2014)
Available anti-malarial tools have over the ten-year period prior to 2012 dramatically reduced the number of fatalities
due to malaria from one million to less than six-hundred and thirty thousand. Although fewer people ...