Now showing items 1-5 of 5
Synthesis, in vitro antiplasmodial activity and cytotoxicity of a series of artemisininetriazine hybrids and hybrid-dimers
A series of artemisininetriazine hybrids and hybrid-dimers were synthesized and their in vitro antimalarial activity against the chloroquine sensitive (CQS), the gametocytocidal (NF54) and the choroquine resistant (CQR) ...
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 ...
Synthesis and in vitro biological activities of ferrocenyl-chalcone amides
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 ...
Synthesis and in vitro biological evaluation of aminoacridines and artemisinin-acridine hybrids
During this study, 9-aminoacridine and artemisinin–acridine hybrid compounds were synthesized and the in vitro for antimalarial activity against both the chloroquine sensitive but also gametocytocidal strain (NF54), and ...
Synthesis, antimalarial activities and cytotoxicities of amino-artemisinin-1,2-disubstituted ferrocene hybrids
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 ...