Neu H C, Fu K P
Antimicrob Agents Chemother. 1980 Aug;18(2):311-6. doi: 10.1128/AAC.18.2.311.
The in vitro activity of three fluorine analogs of chloramphenicol in which the hydroxyl group at position 3 had been replaced with a fluorine was compared with that of chloramphenicol and thiamphenicol. Compound SCH 24893 was the most active agent against staphylococci and Bacteroides strains, and compound SCH 25298 was the most active against Haemophilus, Neisseria, enterococcus, and Klebsiella strains. Serratia marcescens and Pseudomonas aeruginosa strains resistant to chloramphenicol were resistant to the compounds. The agents inhibited all of the Shigella, Salmonella, Staphylococcus aureus, and enterococcus strains resistant to chloramphenicol. They inhibited most (82%) of Escherichia coli and half of the Klebsiella pneumoniae strains which were resistant to chloramphenicol. Isolates in which resistance to chloramphenicol was shown to be plasmic mediated and due to chloramphenicol transacetylase were inhibited by all three agents.
将氯霉素3位羟基被氟取代的三种氟代类似物的体外活性与氯霉素和甲砜霉素进行了比较。化合物SCH 24893对葡萄球菌和拟杆菌菌株活性最强,化合物SCH 25298对嗜血杆菌、奈瑟菌、肠球菌和克雷伯菌菌株活性最强。对氯霉素耐药的粘质沙雷菌和铜绿假单胞菌菌株对这些化合物也耐药。这些药物抑制了所有对氯霉素耐药的志贺菌、沙门菌、金黄色葡萄球菌和肠球菌菌株。它们抑制了大多数(82%)对氯霉素耐药的大肠杆菌菌株以及一半对氯霉素耐药的肺炎克雷伯菌菌株。对氯霉素耐药经质粒介导且由氯霉素转乙酰酶引起的分离株被所有三种药物抑制。