Search
Now showing items 1-10 of 14
In-vitro transdermal penetration of cytarabine and its N4-alkylamide derivatives
(Wiley, 2010)
Objectives The aim of this study was to synthesise and determine the transdermal penetration of cytarabine alkylamide derivatives and assess the correlation of flux with physicochemical properties.
Methods The alkylamide ...
Artemisinin quinoline hybrid-dimers: synthesis and in vitro antiplasmodial activity
(Elsevier, 2010)
Novel artemisinin–quinoline hybrid-dimers were synthesized from dihydroartemisinin and different aminoquinolines at elevated temperatures (90–110 °C). All compounds were obtained as the β-isomers and were tested against ...
Synthesis and in vitro antimalarial activity of a series of bisquinoline and bispyrrolo[1,2a]quinoxaline compounds
(Elsevier, 2012)
Series of bisquinolines 4e15 and bispyrrolo[1,2a]quinoxalines 16e20 containing various polyamine
linkers were synthesized. The aqueous solubility and distribution coefficient were experimentally
determined. The compounds ...
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 ...
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 ...