IN WHICH X REPRESENTS ORYGEN OR SULFUR, R1 REPRESENTS HALOGEN, TRIFLUOROMETHYL, NITRO, ALKYL OF 1 TO 4 CARBON ATOMS, ALKOXY OF 1 TO 4 CARBON ATOMS OR HALOGEN-ALKOXY OF 1 TO 4 CARBON ATOMS, OR, IF X STANDS FOR SULFUR, R1 STANDS FOR HYDROGEN, AND R2 REPRESENTS HYDROGEN OR THE SUBSTITUENTS GIVEN FOR R1, WICH COMPOUND HAS INTERESTING CHEMOTHERAPEUTICAL PROPERTIES AND IS EFFECTIVE AGAINST INTESTINAL WORMS AS HELMINTHS, ESPECIALLY AGAINST LIVER FLUKES. BECAUSE OF THEIR ANTIMYCOTIC PROPERTIES, THE COMPOUNDS OF THE INVENTION MAY ALSO BE USED IN HUMAN MEDICINE AND IN VETERINARY MEDICINE TO ATTACK FUNGUS INFECTIONS.
Abstract:
WHEREIN R1, R2, R3 AND R4 ARE INDENTICAL OR DIFFERENT AND REPRESENT ALKYL RADICALS HAVING 1 TO 8 CARBON ATOMS, PHENYL RADICALS OR PHENYL RADICALS SUBSTITUTED BY LOWER ALKYL RADICALS AND R5 REPRESENTS HYDROGEN OR THE METHYL GROUP AND THE USE OF THESE COMPOUNDS FOR THE ANTIMICROBIAL FINISHING OF TEXTILES.
Abstract:
Arylmethylazoles of the formula I I in which Aryl is (substituted) phenyl or naphthyl; Z is CH or N; R1 and Q are H or alkyl; R2 is H, alk(en)yl or alkynyl; R3 and R4 are H, alkyl or other hydrocarbons; or R3 and R4 together are a -(CH2)2-11 chain or a bridged -(CH2)4-5 chain, and their acid addition salts, stereoisomers and optically active enantiomers possess outstanding antimycotic and antidepressant activity. They are obtained, inter alia, from arylmethylazoles II II which are reacted with a strong base and then with a carbonyl compound III O=CR3R4; thereafter, the product is reacted with the protic acid or with an alkyl halide IV R2Hal. If desired, the products are converted to the acid addition salts, or the stereoisomers or optically active enantiomers are resolved.
Abstract:
Compounds I where A equals t-butyl, phenyl, biphenylyl, phenoxyphenyl, benzylphenyl, benzyloxyphenyl, phenylthiophenyl, phenylsulfinylphenyl, phenylsulfonylphenyl, naphthyl, 1,2,3,4-tetrahydronaphthyl, indanyl, fluorenyl, thienyl, furyl, pyridyl, isoxazolyl, pyrazolyl, benzofuryl or benzothienyl, Z equals CO, CH2 or radicals of ketone derivatives; Y equals azole or equals -X-R8 (R8=(cyclo)alkyl or an aromatic) or equals a number of amine derivatives or equal acyl, are antimycotics. The preparation and use as medicaments are described.