- Synthesis and Antimalarial Properties of 1-Imino Derivatives of 7-Chloro-3-substituted-3,4-dihydro-1,9(2H,10H)-acridinediones and Related Structures
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To improve upon the activity and properties of the 3-aryl-7-chloro-3,4-dihydro-1,9(2H,10H)-acridinediones, a variety of 1-imino derivatives (3) were prepared and shown to be highly active antimalarial agents in both rodents and primates.Among structural modifications prepared, including N10-alkyl and C2-substituted analogs, removal of the C9 oxygen, and introduction of an imino side chain at C9, the imines of the N10-H acridinediones were the most active compounds obtained.The imino derivative of7-chloro-3-(2,4-dichlorophenyl)-3,4-dihydro-1,9(2H,10H)-acridinedione (9aa) proved to be highly active in advanced studies in primates.
- Kesten, Stephen J.,Degnan, Margaret J.,Hung, Jocelyn,McNamara, Dennis J.,Ortwine, Daniel F.,et al.
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p. 3429 - 3447
(2007/10/02)
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- 10-Hydroxy-3,4-dihydroacridine-1,9(2H,10H)-diones: a new group of malaricidal and coccidiostatic compounds
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2-Nitrobenzaldehydes and 1,3-cyclohexanediones condense in a mixture of hydrocholic acid and glacial acetic acid to 10-hydroxy-3,4-dihydroacridine-1,9(2H,10H)-diones. Many compounds of this group reveal a pronounced coccidiostatic and malaricidal effect i
- Duerckheimer,Raether,Seliger,Seidenath
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p. 1041 - 1046
(2007/10/02)
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