新型6-位脱氟喹诺酮类抗菌药T-3811ME

T-3811ME,a novel 6-des-fluoro-quinolone antibiotic

6 位氟的引入 ,使喹诺酮类抗菌药的抗菌作用显著增强。而在寻找新的喹诺酮类抗菌药的过程中发现有几个 6 位脱氟喹诺酮化合物较 6 位氟取代化合物有更强的抗菌活性 ,而且毒性更低。其中T 381 1ME在各方面的性质尤为突出。T 381 1ME对金葡球菌、甲氧西林耐药的金葡球菌、青霉素耐药肺炎链球菌、肺炎支原体、结核杆菌、军团菌、厌氧菌等活性优于目前临床使用的 6 氟喹诺酮。T 381 1ME的毒性也较低 。

Introduction of 6 fluoro into quinolone antibacterial agents increased markedly the antibacterial activity.In the search for new antibacterial agents,some of 6 des fluoro quinolone compounds were found more active in antibacterial effects and less toxicity than the corresponding 6 fluoro compounds.In those compounds,T 3811ME showed excellent antibacterial property.Against S.aureus ,MRSA,penicillin resistent S.pneumoniae,Mycoplasma pneumoniae,Mycobacterium tuberculosis,Legionella spp .and anaerobes,it was superior to those 6 fluoro quinolones used in clinic.T 3811ME caused less toxic effects, especially the erosion of articular cartilage in animal than other quinolone antibacterial agents.