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    • 53. 发明专利
    • BENZO[B]THIOPHENES, BENZO[B]FURANS, THIOCHROMANS AND CHROMANS HAVING ANTIMICROBIAL ACTIVITY
    • CA1213591A
    • 1986-11-04
    • CA400570
    • 1982-04-06
    • SCHERING CORP
    • RANE DINANATH FWRIGHT JOHN JPIKE RUSSELL E
    • C07D405/00
    • Compounds of the formula I wherein n is 0 or an integer from 1 to 4; p is 0 or 1; q is 0, 1 or 2, R and R1 are independently hydrogen or halogen atoms, or lower alkyl, halolower alkyl, nitro or NR2R3 groups, wherein R2 and R3 are independently hydrogen atoms or lower alkyl groups; or R and R1 together in adjacent positions complete a fused saturated or unsaturated carbocyclic ring that may contain 5 to 7 carbon atoms; X is an oxygen or sulfur atom or a sulphinyl or sulphonyl group; Y is an imidazolyl or 1,2,4-triazolyl group, either of which may be substituted by a lower alkyl or aryl group, wherein said aryl group is a phenyl, halophenyl or lower alkyl phenyl group; Z is an alkyl, alkenyl, alkynyl, cycloalkyl or heterocyclic aromatic group, which may have at least one substituent selected from halogen atoms and lower alkyl, lower alkoxy, lower alkylidenedioxy, phenyl and N-(N'-lower alkanoylpiperazinyl) groups, provided that, when n is 0, Z is not 1-alkynyl; and, when n is 1 to 4, Z can also be an alkoxy, alkylthio, aryl, aryloxy or arylthio group, or an aryl, aryloxy or arylthio group having substituents selected from halogen atoms and lower alkyl, lower alkoxy, lower alkylidenedioxy and N-(N'-lower alkanoylpiperazinyl) groups; where the term "lower" indicates groups having 1 to 6 carbon atoms; and the broken line indicates a single or double bond, with the proviso that it is a double bond only when p is 0 and X is a sulfur atom; and the acid addition salts thereof; have antimicrobial, in particular antifungal, antibacterial and antiprotozoal activity. Compositions, especially pharmaceutical compositions, containing them and processes for their preparation are also disclosed.