The trypanocidal action of some derivatives of anil and styryl quinoline

Abstract

As tested on mice infected with Trypanosoma brucei, the most marked trypanocidal action was exerted by substances which contained a free basic group in one nucleus and an acylamino group in the other, especially in the styryl series. The compounds, 2([image]-amino styryl) -6 acetylamino quinoline methochloride and 2([image]-acetyl-amino styryl) -6 dimethylamino quinoline methochloride, were the most active substances, cures being occasionally produced by 1/50 of the maximum tolerated dose. Cures resulted even when 1/3 of the tolerated dose was administered to mice in a moribund condition whose blood was swarming with parasites. Very little prophylactic action was exerted by the latter substance and it was inactive when ingested per os. In vitro it had only slight lethal action on trypanosomes. Drug-resistant strains were developed by the usual method; they were also resistant to arsacetin, tryparosan and trypaflavin but not to trypanblue and Bayer 205. Rabbits treated 3 to 5 weeks after inoculation with T. brucei, when definite symptoms had developed, were cured in most cases by a single dose of either substance administered subc. The chemical preparations of the substances are described.