Synthesis and antibacterial activity of 1beta-methyl-2-(5-substituted thiazolo pyrrolidin-3-ylthio)carbapenem derivatives.
The synthesis of a new series of 1beta-methylcarbapenems having the substituted thiazolopyrrolidine moiety is described. Their in vitro antibacterial activities against both Gram-positive including MRSA and Gram-negative bacteria were tested and the effect of substituent on the thiazole ring was investigated. A particular compound (28c) having 4'-amide substituted thiazole moiety showed the most potent antibacterial activity.
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry; D001419:Bacteria / Q000187:drug effects*; D015780:Carbapenems / Q000138:chemical synthesis* / Q000737:chemistry; D004150:Dipeptidases / Q000378:metabolism; D007202:Indicators and Reagents; D007668:Kidney / Q000201:enzymology; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D016106:Methicillin Resistance; D008826:Microbial Sensitivity Tests; D013055:Spectrophotometry, Infrared; D013056:Spectrophotometry, Ultraviolet; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D015780:Carbapenems; D007202:Indicators and Reagents; D004150:Dipeptidases; C038937:dipeptidase