摘要:
4-(1''-ALKYL-5''-NITROIMIDAZOLYL-2''-METHYLENE-IMINO)-TETRAHYDRO1,4-THIAZINE 1,1-DIOXIDES OF THE FORMULA
IN WHICH R1 is hydrogen, methyl, ethyl, or 2-hydroxy-ethyl and R2 is hydrogen, methyl, ethyl or methoxymethyl, are prepared by reaction of 1-alkyl-5-nitroimidazolyl-2-aldehyde or a functional derivative thereof with 4-amino-tetrahydro-1,4-thiazine 1,1dioxide. The products of the invention are suitable for the treatment of protozoal diseases.
摘要:
1-(PYRIDYL-THIOALKYL)-2-ALKYL-5-NITRO-IMIDAZOLES OF THE FORMULA
IN WHICH R1 is hydrogen, methyl or ethyl, -(CH2)n- is an alkyl chain of 2 to 4 carbon atoms which may be branched and to which the pyridyl group is linked in 2-, 3- or 4-position via a sulfur atom, are prepared by reaction of 1-( omega -halogeno-alkyl)-2alkyl-5-nitro-imidazole with mercapto-pyridine in the presence of an acid-binding agent or by reaction of 2-alkyl-5-nitro-imidazole with omega -halogeno-alkyl-thio-pyridine in the presence of an acid-binding agent or with omega -hydroxy-alkyl-thio-pyridine in the presence of a condensation agent or with an aryl-sulfonyloxyalkyl-thio-pyridine. The products of the invention are suitable for the treatment of protozoal diseases.
摘要:
Formamidine derivatives of diphenyl-sulfone which are effective medicaments against malaria are prepared by reacting 4,4'' diamino-diphenyl-sulfone of the formula
WITH N-formyl compounds of the formula
IN WHICH -N Z is a pyrrolidino, piperidino or morpholino radical, in the presence of acid halides and, if desired, converting the salts thus obtained into the free bases.
摘要:
(1-Alkyl-5-nitro-imidazolyl-2-alkyl)-pyridyl-sulfides, sulfoxides and -sulfones of the formula I
in which R1 represents methyl or ethyl, R2 represents a hydrogen atom or methyl, Z represents a sulfide group (-S-), a sulf-oxide group (-SO-) or a sulfone group (-SO2-), which may be linked with the pyridine ring in the 2-, 3- or 4-position, and in which R3 represents a halogen atom, a cyano or nitro group, and process for preparing them. The compounds are active against trichomonas and amebas.
摘要:
This invention provides 1-alkyl-2-(pyridylthiomethyl)-5-nitroimidazoles and 1-alkyl-2-(N-oxy-pyridylthiomethyl)-5-nitroimidazoles of the formula
in which R is methyl, ethyl or hydroxyethyl and the pyridyl and N-oxy-pyridyl group is linked in 2-, 3- or 4-position to the sulfur atom, as well as process for the manufacture of these compounds. The novel compounds are suitable for the treatment of protozoal diseases in mammals.
摘要:
1,4-BIS-(5''-NITROIMIDAZOLYL-2''-METHYLENE-IMINO) PIPERAZINES OF THE FORMULA
IN WHICH R1 is hydrogen, methyl, ethyl or 2-hydroxyethyl and R2 is hydrogen or methyl, are prepared by reaction of 5-nitroimidazolyl-2-aldehydes or the functional derivatives thereof with 1,4-diamino-piperazines. The products of the invention are suitable for the treatment of protozoal diseases.
摘要:
New 1-alkyl-2-(pyridyl-sulfinylmethyl)-5-nitro-imidazoles and 1alkyl-2-(pyridyl-sulfonylmethyl)-5-nitro-imidazoles are described according to the formula I
in which R stands for a methyl, ethyl or hydroxyethyl group and Z stands for a -SO- or -SO2- group and the pyridine ring is linked to the sulfinyl or the sulfonyl group in 2, 3 or 4 position as well as a process for their manufacture. The novel compounds have a pronounced activity against protozoae, especially trichomonads and amebae.