Antiprotozoal (1)-methyl-(2)-phenoxymethyl-(5) nitro-imidazoles - prepd. e.g. by reacting (2)-halomethyl cpds. with substd. phenols

摘要

New 1-methyl-2-(phenoxymethyl)-5-nitro-imidazole derivs. are of formula (I). In (I) R1 is NO2, CN, methylsulphonyl or ethylsulphonyl; and R2 is methyl or halogen. (I) are useful against e.g., trichomoniasis, amoebiasis, and tripanosomiasis. They can be administered orally or locally. The activity of (I) against trichomonads and amoebae is better than that of the known agent metronidazole. Specific cpds. (I) include 1-methyl-2-(3-methyl-4-nitrophenoxymethyl)-5-nitroimidazole. In an example, this is prepd. by suspending 17.6 g. 1-methyl-2-chloromethyl-5-nitroimidazole and 15.1 g. 3-methyl-4-nitrophenol in 80 ml. acetone, adding 13.8 g. powdered K2SO3 and stirring 2 hrs. at 50-60 degrees C.