Search
Now showing items 1-10 of 10
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 ...
Synthesis, in vitro antimalarial activity and cytotoxicity of novel 4-aminoquinolinyl-chalcone amides
(Elsevier, 2014)
A series of 4-aminoquinolinyl-chalcone amides 11–19 were synthesized through condensation of carboxylic
acid-functionalized chalcone with aminoquinolines, using 1,10-carbonyldiimidazole as coupling
agent. These compounds ...
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 ...
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 ...
Synthesis and in vitro biological evaluation of aminoacridines and artemisinin-acridine hybrids
(Elsevier, 2014)
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 ...
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 ...
Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin
(Elsevier, 2016)
In an attempt to improve the efficacy and stability of current, clinically used artemisinins, a series non-hemiacetal ester derivatives of artemisinin were synthesized and evaluated for their in vitro antiplasmodial and ...
Synthesis and in vitro biological evaluation of dihydroartemisinyl-chalcone esters
(Elsevier, 2015)
A series of dihydroartemisinyl-chalcone esters were synthesized through esterification of chalcones with dihydroartemisinin (DHA). The hybrids were screened against chloroquine (CQ) sensitive (3D7) and CQ resistant (W2) ...
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 ...
Synthesis, in vitro antimalarial activities and cytotoxicities of amino-artemisinin-ferrocene derivatives
(Elsevier, 2018)
Novel derivatives bearing a ferrocene attached via a piperazine linker to C-10 of the artemisinin nucleus were prepared from dihydroartemisinin and screened against chloroquine (CQ) sensitive NF54 and CQ resistant K1 and ...