The invention relates to novel 1,2-disubstituted-4-nitroimidazole compounds being useful as potent antiprotozoal agents which possess non-mutagenic activity. The novel compounds disclosed herein are useful in formulating compositions comprising an effective amount of said novel compounds and methods of administering said compositions.
Nitroimidazoles are a class of known compounds and have the reputation as mutagens. Metronidazole (flagyl), a 5-nitro-imidazole is mutagenic and consequently raises concern over safety when administered to patients. Also, the compound, 1-methyl-2-methylsulfonyl-4-nitroimidazole is a known compound and is disclosed in the Indian Journal of Chemistry, Section B, 21B (11), pp. 1006-21. The utility of this compound was disclosed as being active as radio and chemosensitizers and no mention was made of any biological activities or relative mutagenicity. The novel compounds disclosed in the invention herein are not mutagenic in Ames strain TA100, and are highly potent against protozoal diseases and, therefore, offer a greater safety advantage to patients. Said novel compounds are of particular use against Trichomonas spp. such as T. foetus and T. vaginalis.
USPTO Backgrounds
USPTO Backgrounds