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    • 5. 发明授权
    • Broad-spectrum isothiazole antimicrobial agents
    • 广谱异噻唑抗菌药
    • US5508417A
    • 1996-04-16
    • US200254
    • 1994-02-23
    • Peter Osei-GyimahBarry C. Lange
    • Peter Osei-GyimahBarry C. Lange
    • A01N43/80C07D275/02C07D275/03A61K31/425C07D409/12
    • C07D275/03A01N43/80
    • This invention relates to antimicrobial compounds of formula I, II, or III ##STR1## wherein R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, or (C.sub.1 -C.sub.4)alkyl;R.sub.1 and R.sub.2 may be taken together with the carbons to which they are attached to form a 5 to 7-membered carbocyclic ring and the ring may be aromatic;R.sub.3 is hydrogen, (C.sub.1 -C.sub.8)alkyl, (C.sub.2 -C.sub.8)alkenyl, (C.sub.5 -C.sub.8)alkynyl, (C.sub.5 -C.sub.7)cycloalkyl or cycloalkenyl, phenyl or substituted phenyl, (C.sub.7 -C.sub.10)aralkyl or substituted (C.sub.7 -C.sub.10)aralkyl, or a 5 to 8-membered heteroaryl having one or more heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen;R.sub.4 is an electron-withdrawing group selected from CN, NO.sub.2, P(O)(OR.sub.7).sub.2, P(S)(OR.sub.7).sub.2, COOR.sub.6, COR.sub.6, CONHR.sub.6, SOR.sub.6, SO.sub.2 R.sub.6, where R.sub.6 is hydrogen, (C.sub.1 -C.sub.8)alkyl, phenyl or substituted phenyl, (C.sub.7 -C.sub.10)aralkyl or substituted (C.sub.7 -C.sub.10)aralkyl, (C.sub.5 -C.sub.7)cycloalkyl, or a 5 to 8-membered heteroaryl having one or more heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen and where R.sub.7 is (C.sub.1 -C.sub.4)alkyl or phenyl;R.sub.3 and R.sub.4 may be joined to form a (C.sub.5 -C.sub.7)cycloalkenone optionally containing a heteroatom selected from the group consisting of oxygen, sulfur and nitrogen;R.sub.5 is hydrogen or (C.sub.1 to C.sub.4)alkyl; andY is oxygen, sulfur, sulfoxide, sulfone, or nitrogen substituted with (C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.5)cycloalkyl, or phenyl.
    • 本发明涉及式I,II或III的抗微生物化合物,其中R 1和R 2独立地选自氢,卤素或(C 1 -C 4)烷基; R 1和R 2可以与它们所连接的碳一起形成5至7元碳环并且该环可以是芳族的; R3是氢,(C1-C8)烷基,(C2-C8)烯基,(C5-C8)炔基,(C5-C7)环烷基或环烯基,苯基或取代的苯基,(C7-C10)芳烷基或取代的(C7- C10)芳烷基或具有一个或多个选自氧,硫和氮的杂原子的5至8元杂芳基; R4是选自CN,NO2,P(O)(OR7)2,P(S)(OR7)2,COOR6,COR6,CONHR6,SOR6,SO2R6的吸电子基团,其中R6是氢,(C1-C8 )烷基,苯基或取代的苯基,(C 7 -C 10)芳烷基或取代的(C 7 -C 10)芳烷基,(C 5 -C 7)环烷基或具有一个或多个选自氧的杂原子的5至8元杂芳基 ,硫和氮,其中R 7是(C 1 -C 4)烷基或苯基; R 3和R 4可以连接形成任选地含有选自氧,硫和氮的杂原子的(C5-C7)环烯酮; R5是氢或(C1-C4)烷基; 并且Y是被(C 1 -C 4)烷基,(C 3 -C 5)环烷基或苯基取代的氧,硫,亚砜,砜或氮。