Antimalarial drugs. 64. Synthesis and antimalarial properties of 1-imino derivatives of 7-chloro-3-substituted-3,4-dihydro-1,9(2H,10H)-acridinediones and related structures

Autor:	Hung Jocelyn H, Leslie M. Werbel, Margaret J. Degnan, Daniel F. Ortwine, Dennis Joseph Mcnamara, Susan E. Uhlendorf, Stephen J. Kesten
Rok vydání:	1992
Předmět:	Tertiary amine Stereochemistry Chemistry Drug Discovery Side chain Molecular Medicine Biological activity Antimalarial Agent
Zdroj:	Journal of Medicinal Chemistry. 35:3429-3447
ISSN:	1520-4804 0022-2623
DOI:	10.1021/jm00097a001
Popis:	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-[(alkylamino)alkylene]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 [3-(N,N- dimethylamino)propyl]imino derivative of 7-chloro-3-(2,4-dichlorophenyl)-3,4-dihydro-1,9(2H,10H)- acridinedione (9aa) proved to be highly active in advanced studies in primates.
Databáze:	OpenAIRE
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