Trypanocidal activity of a 5-substituted 2-nitroimidazole compound (Ro 15-0216) in mice
Zweygarth, E.; Röttcher, D.
Tropical Medicine and Parasitology Official Organ of Deutsche Tropenmedizinische Gesellschaft and of Deutsche Gesellschaft für Technische Zusammenarbeit 38(3): 171-174
1987
ISSN/ISBN: 0177-2392 PMID: 3432951 Document Number: 286664
The trypanocidal activity of a 5-substituted 2-nitroimidazole compound (Ro 15-0216, 2-(dimethylamino)-4'-[(1-methyl-2-nitroimidazole-5-yl) methoxy] acetanilid) was tested in stocks of Trypanosoma brucei brucei (CP 462, CP 547), T. b. evansi (KETRI 2443, CP 893), T. vivax (CP 1214), and T. congolense (CP 81) in mice. The trypanosome stocks showed different sensitivities, the Trypanozoon group was most sensitive followed by T. vivax and T. congolense. Administration of the compound in the drinking water was superior to single intraperitoneal injections. CP 547, with reduced sensitivity to Mel B and insensitive to diminazene aceturate was cured by a dose 13 times greater than that necessary for the drug-sensitive stock CP 462, administered in the drinking water. Quinapyramine- (KETRI 2443) and quinapyramine/suramin-resistant (CP 893) stocks of T. b. evansi were eliminated with doses of 63 and 160 mg/kg ip, respectively; to eliminate stock CP 462, 250 mg/kg ip were required. The combination of Ro 15-0216 with suramin showed a synergistic effect in stocks KETRI 2443 and in CP 893, although high doses of suramin were applied in the latter. Synergism of Ro 15-0216 with diminazene aceturate was demonstrated in T. congolense-infected mice.