新型6-位脱氟喹诺酮抗菌剂T-3811Me
刘伍山
(天津药物研究院，天津300193)
[摘要] 6-位氟的引入，使喹诺酮抗菌剂的抗菌作用显著增强。而在寻找新的喹诺酮抗菌剂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-3811ME在各方面的性质尤为突出。T-3811ME对金葡球菌、甲氧青霉素耐药金葡球菌、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-3811ME的毒性也较低，特别是对动物关节软骨的浸蚀较其他喹诺酮抗菌剂要小。
[关键词] T-3811ME；喹诺酮抗菌剂；毒性
T-3811ME, A novel 6-des-floro-quinolone antibiotic
Liu wushan
Tianjin institute of pharmaceutical research
[Abstract] Introduction of 6-floro into quinolone antibacterial agents increased markedly the antibacterial activity. In the search for new antibacterial agents, some of 6-des-floro quinolone compounds were found more active in antibacterial effects and less toxic than the corresponding 6-floro 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-floro quinolones used in clinic. T-3811ME caused less toxic effects, especially the erosion of articular cartilage in animal than other quinolone antibacterial agents.
[Key words] T-3811ME, quinolone antibiotic, toxicity
, http://www.100md.com
(天津药物研究院，天津300193)
[摘要] 6-位氟的引入，使喹诺酮抗菌剂的抗菌作用显著增强。而在寻找新的喹诺酮抗菌剂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-3811ME在各方面的性质尤为突出。T-3811ME对金葡球菌、甲氧青霉素耐药金葡球菌、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-3811ME的毒性也较低，特别是对动物关节软骨的浸蚀较其他喹诺酮抗菌剂要小。
[关键词] T-3811ME；喹诺酮抗菌剂；毒性
T-3811ME, A novel 6-des-floro-quinolone antibiotic
Liu wushan
Tianjin institute of pharmaceutical research
[Abstract] Introduction of 6-floro into quinolone antibacterial agents increased markedly the antibacterial activity. In the search for new antibacterial agents, some of 6-des-floro quinolone compounds were found more active in antibacterial effects and less toxic than the corresponding 6-floro 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-floro quinolones used in clinic. T-3811ME caused less toxic effects, especially the erosion of articular cartilage in animal than other quinolone antibacterial agents.
[Key words] T-3811ME, quinolone antibiotic, toxicity
, http://www.100md.com