| 摘要 |
The invention provides compounds of the formula <IMAGE> (I) wherein X is CH2, S or O; R1 is a 3 position substituent such as hydrogen, hydroxy, halo, trifluoromethyl, C2F5, C1-C6 alkyl, C1-C6 substituted alkyl, C1-C6 alkenyl, C1-C6 alkynyl, CH2O(CO)R', CH2O(CO)NH2, CO2R', thio(C1-C6)alkyl, thio(C1C6)alkenyl, oxo(C1-C6)alkyl, phosphine oxide, quaternary ammonium group, substituted or unsubstituted thiazolothio, or oxo(C1-C6)alkenyl; wherein R' is hydrogen, C1-C6 alkyl, or C1-C6 alkenyl; R2 is hydrogen or a carboxy protecting group; R3 is <IMAGE> (CH2)n; wherein R6 is hydrogen Me, CH2F, CF3, C2H5, CH2CH2F, CH2CF3, C2F5, CH2CO2R', CH2CONH2, C(Me)2CO2R', or C(Me)2CONH2; and n is 0-5; R4 is <IMAGE> wherein Z is O, S, NH, or CH2; Y is CH or N; and R7 is hydrogen, C1-C6 alkyl, CONH2, or CO2R'; and R5 is <IMAGE> wherein R8 is CH, N, COH, CO(C1-C6 alkyl) CSH, or CNH2; and R9 is R8 as defined; said R5 optionally substituted 1-4 times with halo, OH, SH, NH2, NO2, CH3, C2H5, CO2R', CONH2, SO3H, or SO2NHR'; and salts thereof. Also, pharmaceutical formulations and methods for treating bacterial infections in man or other animals using the above compounds are disclosed.
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