Abstract
The causal prophylactic and blood schizontocidal action of six dihydroacridinediones were assessed in mice using the Plasmodium yoelii 17X strain in sporozoite-induced infections and the P. berghei K 173 strain in blood-induced infections respectively. A remarkable relationship was shown between the action on pre-erythrocytic forms and on blood forms of malaria parasites. A trifluoromethyl group in the para (4—) position of the 3-phenyl ring of the 7-chloro-10-hydroxy-3,4-dihydroacridine-1,9-(2H,10H)-dione (compound Hoe 991: floxacrine) proved the most favourable substituent of a group of electronegative substituents concerning antimalarial activity. The CPD50/CD50 of Hoe 991 against pre-erythrocytic/blood forms of P.yoelii/P. berghei was 0·37 mg kg−1 (X 1)/1·7 mg kg−1 (X5) after the intraperitoneal (ip)/subcutaneous (sc) route. As demonstrated by compound Hoe 990 double substitution in the 3-phenyl ring with 2-chloro-, 4-trifluoromethyl- caused a marked residual action. The causal prophylactic effect (CP...
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