Experimental therapy of filariasis with furapyrimidone

It was found in animal tests that furapyrimidone, 1-[(5-nitrofurayl-2) methylene amino]tetrahyraopyrimidone-2-one, was an effective antifilarial agent. When cotton rats infected with Litomosoidescarinii were treated orally with furapyrimidone in the daily dose of 25 mg/kg for 5 consecutive days, all adult worms in the pleural cavity were killed. If the daily dose was increased to 100 mg/kg, the microfilariae in the peripheral blood were eradicated. When given orally to Mongolian jirds infected with Brugia malayi in the daily dose of 100-188 mg/kg for 5 consecutive days, part of the adult worms and a greater part of microfilariae in the peritoneal cavity as well as in the peripheral blood were killed. The LD50 in mice treated orally with a single dose of furapyrimidone was 243±31 mg/kg. When the drug was given to dogs at 25 or 75 mg/kg for 4-7 days, only the 75 mg/kg group exhibited some mild vomiting and a decrease of food intake. The histopathological lesions were of little importance.