Furet Y X, Pechère J C
Department of Microbiology, Centre Médical Universitaire, Geneva, Switzerland.
Eur J Clin Microbiol Infect Dis. 1991 Apr;10(4):249-54. doi: 10.1007/BF01966997.
The improved antimicrobial activity of newer fluoroquinolones and novel applications recently found for the drugs already marketed are reviewed. Several new compounds are more active against gram-positive bacteria than the presently marketed fluoroquinolones. WIN 57273, the most potent compound in vitro on a weight basis, is 16 to 128 times more active than ciprofloxacin against various staphylococci, streptococci, Enterococcus spp., Corynebacterium spp., Listeria monocytogenes and Bacillus spp. BMY 40062, PD 117558, PD 127391, sparfloxacin, temafloxacin and tosufloxacin also show enhanced in vitro efficacy against these species. These drugs also possess increased activity against various anaerobes, notably Clostridium perfringens, Clostridium difficile and the Bacteroides fragilis group. Mycobacterium tuberculosis, rapidly growing mycobacteria other than Mycobacterium chelonae, and Mycobacterium leprae are often susceptible to quinolones displaying bactericidal activity which is potentially useful for curing difficult-to-treat mycobacteriosis. In addition, a number of new products, notably those containing a cyclopropyl group, are more active than reference fluoroquinolones against Mycobacterium leprae. Sparfloxacin, BMY 40062 and WIN 57273 compare favorably with older fluoroquinolones in the killing of intracellular Legionella spp., and several of the newer compounds have greater antichlamydial potency. Improved antibacterial activity has also been found against Mycoplasma hominis, Ureaplasma urealyticum, Acinetobacter spp. and Pseudomonas maltophilia. By contrast, the newer quinolones have similar or less activity against Pseudomonas aeruginosa and Enterobacteriaceae. Recently, pefloxacin, ofloxacin and ciprofloxacin were found to be active against protozoa, including Plasmodium spp., Trypanosoma cruzi and Leishmania donovani, but not against Toxoplasma gondii. In the near future, more specific research testing unusual pathogens may lead to the identification of quinolones with more selective activity.
本文综述了新型氟喹诺酮类药物抗菌活性的改善情况以及近期已上市药物的新应用。几种新化合物对革兰氏阳性菌的活性比目前市场上销售的氟喹诺酮类药物更强。以重量计，体外活性最强的化合物WIN 57273对各种葡萄球菌、链球菌、肠球菌属、棒状杆菌属、单核细胞增生李斯特菌和芽孢杆菌属的活性比环丙沙星高16至128倍。BMY 40062、PD 117558、PD 127391、司帕沙星、替马沙星和妥舒沙星对这些菌种也显示出增强的体外疗效。这些药物对各种厌氧菌的活性也有所增加，特别是产气荚膜梭菌、艰难梭菌和脆弱拟杆菌群。结核分枝杆菌、除龟分枝杆菌外的快速生长分枝杆菌以及麻风分枝杆菌通常对具有杀菌活性的喹诺酮类药物敏感，这可能有助于治疗难治性分枝杆菌病。此外，一些新产品，特别是含有环丙基的产品，对麻风分枝杆菌的活性比对照氟喹诺酮类药物更强。在杀灭细胞内嗜肺军团菌方面，司帕沙星、BMY 40062和WIN 57273比旧的氟喹诺酮类药物更具优势，并且几种较新的化合物具有更强的抗衣原体效力。对人型支原体、解脲脲原体、不动杆菌属和嗜麦芽窄食单胞菌也发现了抗菌活性的改善。相比之下，新型喹诺酮类药物对铜绿假单胞菌和肠杆菌科的活性相似或较低。最近发现，培氟沙星、氧氟沙星和环丙沙星对包括疟原虫属、克氏锥虫和杜氏利什曼原虫在内的原生动物有活性，但对弓形虫无活性。在不久的将来，针对不常见病原体的更具体研究测试可能会导致鉴定出具有更具选择性活性的喹诺酮类药物。
