Amidine derivatives are highly effective against Trypanosoma evansi trypomastigotes.
The in vitro effect of N,N'-diphenyl-4-R-benzamidine (where R = H, CN, Br, Cl, CH3, OCH3 and NO2) in three isolates of Trypanosoma evansi was studied. The compounds were solubilized in dimethysulphoxide (DMSO) and tested in a concentration range of 5 to 160 micrograms/ml. The parasites were isolated from a horse, a dog and a coati. They were maintained in immunosuppressed rats, since they could not be cultured in vitro, and further purified through a diethylaminoethanol (DEAE) column. The trypomastigotes obtained were mixed with different concentrations of the drugs and after incubation at 26 degrees C for 24 h, the remaining parasites were counted in a Neubauer chamber. The percentage of inhibition was evaluated compared with the control, without the drugs. Most of the amidine derivatives showed high activity against the three T. evansi isolates, but different patterns of sensitivity to the tested compounds were observed. At least four compounds with Br, Cl, OCH3 and NO2 as substituents, were much more effective than Berenil [4,4'-(diazoamine)-dibenzamidine aceturate], the reference drug used, which is included in the same chemical class of amidines.
Gomes-Cardoso
L
L
Departamento de Imunologia, Instituto Oswaldo Cruz, Rio de Janeiro, Brasil.
Echevarria
A
A
Aguiar-Alves
F
F
Jansen
A M
AM
Leon
L L
LL
D000818:Animals; D001550:Benzamidines / Q000494:pharmacology* / Q000633:toxicity; D004285:Dogs; D006736:Horses; D007928:Lethal Dose 50; D051381:Rats; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000494:pharmacology*; D014345:Trypanosoma / Q000187:drug effects*
D001550:Benzamidines; D014344:Trypanocidal Agents