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US 4,010,176 AGranted
Isoxazole substituted nitroimidazoles
AssigneeMerck & Co., Inc.
InventorsPeter Kulsa, Clarence S. Rooney
Life of this patent
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Abstract
Novel substituted nitroimidazoles are provided, for example, 2-(4,5-substituted-isoxazol-3-yl)-1-substituted-5-nitroimidazole; 2-(4,5-disubstituted-.DELTA..sup.2 -isoxazolin-3-yl)-1-substituted-5-nitroimidazole; or 2-(4,5-disubstituted-2-loweralkyl-isoxazolidin-3-yl)-1-substituted-5-nitro imidazole. These compounds have antibacterial and antiprotozoal activity, especially against human and animal trypanosomiasis and trichomoniasis.
Claims2
A 1,2-disubstituted 5-nitroimidazole having the following structure:
- ##STR40## wherein R.sub.1 is hydrogen, loweralkyl having 1 to 6 carbon atoms, or CH.sub.2 --CH.sub.2 -OH and R is ##STR41## wherein R.sub.4 and R.sub.5 are the same or different and are each hydrogen, loweralkyl having 1-6 carbon atoms, carboxyalkyl, carboxamido, carboxamidoalkyl, carboxamidodialkyl, amino, phenyl, aminoalkyl, or aminodialkyl wherein the alkyl group is carboxyalkyl, carboxamidoalkyl, carboxamidodialkyl, aminoalkyl and aminodialkyl contains 1 to 6 carbon atoms;
- or R.sub.4 and R.sub.5 are a ring structure of:
- (CH.sub.2).sub.n, n being an integar from 3-10;
- provided that when only one of R.sub.4 and R.sub.5 are hydrogen, the substituent other than hydrogen is in the 5-position of the ring.
1 more element
Dependencies are inferred from the claim text.