| 摘要 |
<p>Ceph-3-em-4-carboxylic acid and 2,2-dimethyl-penam-3-carboxylic acid derivatives of the general formula (I), wherein: R<6>R<7>N- or R<6>R<7>-NR<4>-, X is -C(CH3)2-, -CH2-C(CH3)= -CH2-C(CH2OAc)= or -CH2-C(CH2SHet)=, Het is a 5-7 membered heterocyclic group containing 1-4 nitrogen atom(s) and optionally one or more other hetero atom(s), optionally condensed with one or more phenyl group(s) and/or substituted with one or more alkyl, aralkyl, aryl, substituted aryl or substituted aralkyl group(s), R<1> is hydrogen atom, a C1-4 alkyl group or a phenyl group bearing optionally a halo, hydroxy, alkoxy or alkyl substituent, R<2> is hydrogen atom, a C1-4 alkyl group or a phenyl group bearing optionally a halo, hydroxy, alkoxy or alkyl substituent, R<3> and R<8> each stand for hydrogen atom, a C1-4 alkyl group or a phenyl group bearing optionally a halo, hydroxy, alkoxy or alkyl substituent, Q represents oxygen, sulfur or selenium atom, R<4> is hydrogen atom, a C1-4 alkyl group or a group -COOR<5>, R<5> being a C1-8 alkyl group, a benzyl group, a benzhydryl group or a phenyl group bearing optionally a halo, hydroxy, alkoxy or alkyl substituent, R<6> is a phenyl group bearing optionally one or more halo, C1-6 alkyl, nitro, alkoxycarbonyl, trifluoromethyl, dialkylamino, hydroxy, carboxylic acid or sulfonic acid substituent(s), a C1-8 alkyl group optionally bearing an alkoxycarbonyl, hydroxyl, dialkylamino or alkoxy substituent, a C3-8 cycloalkyl group, a C2-6 alkenyl group, a naphthyl group, a heteroaryl group, a 3-8 membered heterocyclyl group optionally condensed with one or more phenyl group(s) and/or bearing one or more substituent(s), or an adamantyl group, and R<7> is hydrogen, or R<6> and R<7> form, together with the adjacent nitrogen atom, a 4-8 membered, unsubstituted or substituted heterocyclic group optionally containing one or more additional nitrogen, oxygen or sulfur atom(s) and optionally condensed with one or more phenyl ring(s), Z is hydroxy group, n is zero or one, and t is zero, one or two, and their pharmacologically acceptable salts and biologically active esters possess strong antimicrobial and enzyme inhibiting, particularly antibacterial and beta -lactamase inhibiting effects.</p> |
