Filaricidal effect of 4 (5-nitrofuryl-2) -methylene amino compounds
Xi, Y.R.; Xu, Y.X.; Nie, J.H.; Yan, M.; Zhang, Z.
Zhongguo Yao Li Xue Bao 5(3): 207-211
1984
ISSN/ISBN: 0253-9756 PMID: 6239515 Document Number: 238517
Filaricidal effect of 3 nitrofurans, M-254 (1-[(5-nitrofuryl-2)-methylene amino]-imidazolin-2-one), M-279 (1-[(5-nitrofuryl-2)-methylene amino]-tetrahydropyrimidin-2-one methanol propionate), and M-280 (1-[(5-nitrofuryl-2)-methylene amino]-tetrahydropyrimidin-2-one methanol cyclohexanocarboxylate), were compared with that of furapyrimidone (M-170) (1-[(5-nitrofuryl-2)-methylene amino] tetrahydropyrimidin-2-one). In mice the acute oral LD50 and 95% confidence limits of M-254, M-279, M-280 and M-170 were 556 .+-. 85,556 .+-. 88,730 .+-. 122 and 231 .+-. 21 mg/kg, respectively. The efficacy of M-254 on Litomosoides carinii in cotton rats was superior to that of M-170 on equitoxic basis; all adult worms in the pleural cavity were killed when M-254 was given orally to L. carinii-infected cotton rats at 1/40 LD50 daily for 5 consecutive days while M-170 failed to do so even at 1/20 LD50 level. M-254 was also more effective than M-170 against microfilariae in peripheral blood and peritoneal cavity of Mongolian jirds infected with Brugia malayi, though the 2 compounds were similar in their effects on adult worms in jird as well as microfilariae and adult worms in vitro. M-279 and M-280 were inferior to M-170 in their filaricidal effect.