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Laboratory Studies on 3-Chloro-9-(4-Diethylamino-1-Methylbutylamino) Acridine, 10-Oxide Dihydrochloride (CI-423) as an Antimalarial Compound

This study deals with the compound CI-423 [3-chloro-9(4-diethylamino-1-methylbutylamino) acridine, 10-oxide, dihydrochloride] as a potential non-staining, suppressive antimalarial drug.

Comparative testing by the drug-diet method against trophozoite-induced Plasmodium lophurae infections in chicks indicated CI-423 to be approximately 16 times as active as quinine, 4 times as active as quinacrine, and one-half as active as amodiaquin.

Comparisons on a single or multiple oral dose basis against trophozoite-induced Plasmodium cynomolgi infections in rhesus monkeys showed CI-423 to be distinctly more potent than either amodiaquin or quinacrine in rapidly suppressing the acute parasitemia and curing the animals.

In contrast to quinacrine, CI-423 did not induce visible staining of the skin of mice or rats when given for respective periods of 2 and 4 weeks.

^* Present address: University of Texas Medical Branch, Galveston, Texas.