Mirelis B, Navarro F, Miró E, Coll R, Xicota M A, Prats G
Microbiology Department, Hospital de Sant Pau, Barcelona, Spain.
Drugs Exp Clin Res. 1995;21(4):129-38.
E-4868, (-)-7[3-(R)-amino-2-(S)-methyl-1-azetidinyl]-1-(2,4- difluorophenyl)-1,4-dihydro-6-fluoro-4-oxo-3-quinolinecarboxylic acid, is a new fluoroquinolone with a 7-azetidin ring substituent. The in vitro activity against clinical isolates was compared with that of ciprofloxacin, ofloxacin and fleroxacin. In general, activity of E-4868 against aerobic and facultative anaerobic Gram-negative bacilli was equal to or slightly less active than ciprofloxacin with the exception of Morganella morganii and Proteus spp., E-4868 MIC90, 1 and 0.5 microgram/ml, respectively. E-4868 activity was two- to eight-fold higher than ciprofloxacin against Gram-positive cocci. For anaerobic species, E-4868 activity was comparable to that of ciprofloxacin, although against the Bacteroides fragilis group E-4868 was four-fold more active than ciprofloxacin.
E-4868,即(-)-7-[3-(R)-氨基-2-(S)-甲基-1-氮杂环丁烷基]-1-(2,4-二氟苯基)-1,4-二氢-6-氟-4-氧代-3-喹啉羧酸,是一种带有7-氮杂环丁烷环取代基的新型氟喹诺酮类药物。将其对临床分离株的体外活性与环丙沙星、氧氟沙星和氟罗沙星进行了比较。总体而言,E-4868对需氧和兼性厌氧革兰氏阴性杆菌的活性与环丙沙星相当,或略低于环丙沙星,但摩根氏摩根菌和变形杆菌属除外,E-4868的MIC90分别为1微克/毫升和0.5微克/毫升。E-4868对革兰氏阳性球菌的活性比环丙沙星高两到八倍。对于厌氧菌种,E-4868的活性与环丙沙星相当,尽管对脆弱拟杆菌群,E-4868的活性比环丙沙星高四倍。