243989-41-5Relevant academic research and scientific papers
"One-pot" synthesis and antimalarial activity of formamidine derivatives of 4-anilinoquinoline
Delarue, Sandrine,Girault, Sophie,Dali Ali, Fouad,Maes, Louis,Grellier, Philippe,Sergheraert, Christian
, p. 933 - 937 (2001)
Amodiaquine (AQ) is an antimalarial which is effective against chloroquino-resistant strains of Plasmodium falciparum but whose clinical use is severely restricted because of associated hepatotoxicity and agranulocytosis. "One-pot" synthesis of formamidin
Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline
Delarue-Cochin, Sandrine,Grellier, Philippe,Maes, Louis,Mouray, Elisabeth,Sergheraert, Christian,Melnyk, Patricia
, p. 2045 - 2055 (2008/12/22)
A series of 4-anilinoquinolines bearing an amino side chain linked to the aromatic ring with a carbamate or an amide bond were synthesized and evaluated for their antimalarial activity and their cytotoxicity upon MRC-5 cells. Among the 17 compounds, a majority was found to be active in the low nanomolar range against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro with relative low cytotoxicity. Two compounds were then tested on mice infected by Plasmodium berghei and were found to exhibit reasonable in vivo activity.
Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines
Delarue,Girault,Maes,Debreu-Fontaine,Labae?d,Grellier,Sergheraert
, p. 2827 - 2833 (2007/10/03)
A new series of 4-anilinoquinolines with two proton-accepting side chains has been synthesized. Antimalarial activity and levels of cytotoxicity upon both MRC-5 cells and macrophages were found to be highly dependent upon the features of these side chains
