| 摘要 |
<p>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-β-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 R1 represents lower alkyl or optionally protected hydroxy lower alkyl; R?2, R13 and R14¿ represent each hydrogen or lower alkyl; R3 represents optionally esterified carboxyl; R?4, R9, R10 and R15¿ represent each an amino-protective group, hydrogen or lower alkyl; R?5, R6, R11 and R12¿ represent each hydrogen, hydroxyl, lower alkyl, hydroxy lower alkyl or halogen, or alternatively R?5 and R6¿ and/or R?11 and R12¿ may combine together to form alkylene; R7 represents hydrogen, lower alkyl, carboxyl, carbamoyl or -CONR?71R72; R71 and R72¿ represent each hydrogen or lower alkyl; R8 represents hydrogen, lower alkyl or hydroxy lower alkyl, or alternatively R8 may combine with R7 to form alkylene; Z represents a single bond, oxygen, sulfur, -CR?11R12-, -NR13¿CO-, -CONR14- or -NR15-; and m and n represent each an integer of 0 to 6.</p> |
