CARBAPENEM DERIVATIVE

摘要

Known carbapenem derivatives such as thienamycin have disadvantages that they are physicochemically unstable and readily decomposed by enzymes such as DHP of the kidney to bring about adverse effects such as nephrotoxicity, while 1- beta - methylcarbapenem compounds are stable and have potent antibacterial activities but are yet unsatisfactory as regards the stability and antibacterial activity against DHP. Under these circumstances the invention provides an antibiotic represented by general formula (I) which has a potent antibacterial activity against various bacteria including Pseudomonas aeruginosa and is excellent in safety and stable against hydrolases such as DHP, and a salt thereof (I), wherein R<1> represents lower alkyl or optionally protected hydroxy lower alkyl; R<2>, R<1><3> and R<1><4> represent each hydrogen or lower alkyl; R<3> represents optionally esterified carboxy R<4>, R<9>, R<1><0> and R<1><5> represent each an amino-protective group, hydrogen or lower alkyl; R<5>, R<6>, R<1><1> and R<1><2> represent each hydrogen, hydroxyl, lower alkyl, hydroxy lower alkyl or halogen, or alternatively R<5> and R<6> and/or R<1><1> and R<1><2> may combine together to form alkylene; R<7> represents hydrogen, lower alkyl, carboxyl, carbamoyl or -CONR<7><1>R<7><2>; R<7><1> and R<7><2> represent each hydrogen or lower alkyl; R<8> represents hydrogen, lower alkyl or hydroxy lower alkyl, or alternatively R<8> may combine with R<7> to form alkylene; Z represents a single bond, oxygen, sulfur, -CR<1><1>R<1><2>-, -NR<1><3>CO-, -CONR<1><4>- or -NR<1><5>-; and m and n represent each an integer of 0 to 6.