102192-73-4Relevant academic research and scientific papers
Antimalarial and anticoccidial activity of 3-aryl-7-chloro-3,4-dihydroacridine-1,9-(2H,10H)-diones. 1-Imines, 1-amines, 1-oximes, 1-hydrazones and related compounds
Winkelmann,Raether
, p. 647 - 661 (2007/10/02)
Out of more than 130 synthesized derivatives of floxacrine and of 10-deoxyfloxacrine, such as 3-(4-trifluoromethyl-phenyl) or 3-(4-chlorophenyl)-7-chloro-10-hydroxy- or -10-deoxy-3,4-dihydroacridine-1,9(2H,10H)-dione 1-imines and 1-hydrazones, more than 4
3-Acryl-7-chloro-3,4-dihydro-1,9(2H, 19H) acridinedione, 1-hydrazones as potent antimalarial agents (1,2)
Werbel,Hung,McNamara,Ortwine
, p. 363 - 370 (2007/10/02)
A series of 3-aryl-7-dihydro-1,9(2H, 10H)-acridinedione, 1-hydrazones was prepared from the corresponding acridinediones, and examined for antimalarial activity. Potent antimalarial activity against Plasmodium berghei infections in mice was found with aliphatic substituted hydrazones. Among the substituents on the phenyl ring at the 3 position of the acridine moiety particularly high activity was associated with the 4-(trifluoromethyl)phenyl group and the 2,4-dichlorophenyl group. Moreover the ring N-OH function was shown to be necessary for good biological activity. Additional structure activity relationships are also discussed.
