Schistosomicidal activity of alkylaminooctanethiosulfuric acids.
The schistosomicidal activity of a new series of alkylaminooctanethiosulfuric acids was studied in white Swiss mice infected with the L.E. strain of Schistosoma mansoni (Belo Horizonte, MG, Brazil). In a preliminary screening of six compounds, two derivatives - 2-[(1-methylpropyl)amino]-1-octanethiosulfuric acid and 2-[(1-methylethyl)-amino]-1-octanethiosulfuric acid - given orally in doses of 300 mg/kg/day for five consecutive days, caused interruption of the oviposition and the hepatic shift of more than 90% of the worms. Both compounds caused a significant reduction in worm burden and, interestingly, the female schistosomes were more susceptible. With the therapeutic schedule of two doses of 800 mg/kg over a 20 day interval, the death of almost all the females and about 50% of the males was observed. Female worms recovered from treated mice showed scattered vitteline glands. Results of in vitro experiments against different developmental stages of the parasite revealed the induction of paralysis and damage to the tegument membrane. The drugs presented no toxic effects on the animals.
Penido
M L
ML
Departamento de Bioquimica e Imunologia, Universidade Federal de Minas Gerais, Belo Horizonte, Brasil.
Nelson
D L
DL
Vieira
L Q
LQ
Coelho
P M
PM
D000818:Animals; D005260:Female; D008297:Male; D051379:Mice; D012550:Schistosoma mansoni / Q000378:metabolism; D012555:Schistosomiasis mansoni / Q000378:metabolism*; D012556:Schistosomicides / Q000737:chemistry / Q000378:metabolism*; D013464:Sulfuric Acids / Q000008:administration & dosage / Q000378:metabolism*
D012556:Schistosomicides; D013464:Sulfuric Acids