109637-83-4Relevant articles and documents
Synthesis of water soluble c-10-phenoxy artemisinin-chitosan conjugate
Xiao, Dan,Yang, Bo,Chen, Yun-Jian,Liao, Xia-Li,Yang, Xue-Min,Qin, Qi-Xue,Yi, Dong
, p. 4654 - 4656 (2013)
A sort of C-10-phenoxy artemisinin-chitosan conjugate, in which C-10-phenoxy artemisinin was covalently bound to chitosan, was prepared and its aqueous solubility was evaluated. The results indicated that the conjugate (1.013 mg/mL) had much higher aqueous solubility than artemisinin (0.0084 mg/mL) and C-10-phenoxy artemisinin (0.0245 mg/mL). The conjugate will be potentially useful for their application as the prodrug of artemisinin.
Method and apparatus for the synthesis of dihydroartemisinin and artemisinin derivatives
-
, (2015/02/02)
The present invention is directed to a method for continuous production of dihydroartemisinin and also artemisinin derivatives derived from dihydroartemisinin by using artemisinin or dihydroartemisinic acid (DHAA) as starting material as well as to a continuous flow reactor for producing dihydroartemisinin as well as the artemisinin derivatives. It was found that the reduction of artemisinin to dihydroartemisinin in a continuous process requires a special kind of reactor and a special combination of reagents comprising a hydride reducing agent, at least one activator such as an inorganic activator, at least one solid base, at least one aprotic solvent and at least one C1-C5 alcohol.
Artemisinin-dipeptidyl vinyl sulfone hybrid molecules: Design, synthesis and preliminary SAR for antiplasmodial activity and falcipain-2 inhibition
Capela, Rita,Oliveira, Rudi,Goncalves, Lidia M.,Domingos, Ana,Gut, Jiri,Rosenthal, Philip J.,Lopes, Francisca,Moreira, Rui
scheme or table, p. 3229 - 3232 (2010/05/02)
A series of artemisinin-vinyl sulfone hybrid molecules with the potential to act in the parasite food vacuole via endoperoxide activation and falcipain inhibition was synthesized and screened for antiplasmodial activity and falcipain-2 inhibition. All conjugates were active against the Plasmodium falciparum W2 strain in the low nanomolar range and those containing the Leu-hPhe core inhibited falcipain-2 in low micromolar range.