INVITRO AND INVIVO ANTIBACTERIAL ACTIVITIES OF T-3761, A NEW QUINOLONE DERIVATIVE

被引:37
作者
FUKUOKA, Y
IKEDA, Y
YAMASHIRO, Y
TAKAHATA, M
TODO, Y
NARITA, H
机构
[1] Research Laboratories, Toyama Chemical Co., Ltd., Toyama 930, 2-4-1, Shimookui
关键词
D O I
10.1128/AAC.37.3.384
中图分类号
Q93 [微生物学];
学科分类号
071005 ; 100705 ;
摘要
T-3761, a new quinolone derivative, showed broad and potent antibacterial activity. Its MICs for 90% of the strains tested were 0.20 to 100 mug/ml against gram-positive bacteria, including members of the genera Staphylococcus, Streptococcus, and Enterococcus; 0.025 to 3.13 mug/ml against gram-negative bacteria, including members of the family Enterobacteriaceae and the genus Haemophilus; 0.05 to 50 mug/ml against glucose nonfermenters, including members of the genera Pseudomonas, Xanthomonas, Acinetobacter, Alcaligenes, and Moraxella; 0.025 mug/ml against Legionella spp.; and 6.25 to 25 mug/ml against anaerobes, including Bacteroides fragilis, Clostridium difficile, and Peptostreptococcus spp. The in vitro activity of T-3761 against these clinical isolates was comparable to or 2- to 32-fold greater than those of ofloxacin and norfloxacin and 2- to 16-fold less and 1- to 8-fold greater than those of ciprofloxacin and tosufloxacin, respectively. When administered orally, T-3761 showed good efficacy in mice against systemic, pulmonary, and urinary tract infections with gram-positive and gram-negative bacteria, including quinolone-resistant Serratia marcescens and Pseudomonas aeruginosa. The in vivo activity of T-3761 was comparable to or greater than those of ofloxacin, ciprofloxacin, norfloxacin, and tosufloxacin against most infection models in mice. The activities of T-3761 were lower than those of tosufloxacin against gram-positive bacterial systemic and pulmonary infections in mice but not against infections with methicillin-resistant Staphylococcus aureus. The activities of T-3761 against systemic quinolone-resistant Serratia marcescens and Pseudomonas aeruginosa infections in mice were 2- to 14-fold greater than those of the reference agents.
引用
收藏
页码:384 / 392
页数:9
相关论文
共 16 条
  • [1] INVITRO ACTIVITY OF CIPROFLOXACIN, A NEW CARBOXYQUINOLINE ANTIMICROBIAL AGENT
    ELIOPOULOS, GM
    GARDELLA, A
    MOELLERING, RC
    [J]. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1984, 25 (03) : 331 - 335
  • [2] INVITRO AND INVIVO ANTIBACTERIAL ACTIVITIES OF T-3262, A NEW FLUOROQUINOLONE
    FUJIMAKI, K
    NOUMI, T
    SAIKAWA, I
    INOUE, M
    MITSUHASHI, S
    [J]. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1988, 32 (06) : 827 - 833
  • [3] FUKUOKA Y, 1990, CHEMOTHERAPY TOKYO
  • [4] PHARMACOKINETIC STUDIES OF NORFLOXACIN IN LABORATORY-ANIMALS
    GILFILLAN, EC
    PELAK, BA
    BLAND, JA
    MALATESTA, PF
    GADEBUSCH, HH
    [J]. CHEMOTHERAPY, 1984, 30 (05) : 288 - 296
  • [5] COMPARATIVE ANTIBACTERIAL ACTIVITIES OF TEMAFLOXACIN HYDROCHLORIDE (A-62254) AND 2 REFERENCE FLUOROQUINOLONES
    HARDY, DJ
    SWANSON, RN
    HENSEY, DM
    RAMER, NR
    BOWER, RR
    HANSON, CW
    CHU, DTW
    FERNANDES, PB
    [J]. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1987, 31 (11) : 1768 - 1774
  • [6] INVITRO ANTI-BACTERIAL ACTIVITY OF AM-715, A NEW NALIDIXIC-ACID ANALOG
    ITO, A
    HIRAI, K
    INOUE, M
    KOGA, H
    SUZUE, S
    IRIKURA, T
    MITSUHASHI, S
    [J]. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1980, 17 (02) : 103 - 108
  • [7] INVITRO ACTIVITY OF AT-4140 AGAINST QUINOLONE-RESISTANT AND METHICILLIN-RESISTANT STAPHYLOCOCCUS-AUREUS
    KOJIMA, T
    INOUE, M
    MITSUHASHI, S
    [J]. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1990, 34 (06) : 1123 - 1127
  • [8] LITCHFIELD JT, 1949, J PHARMACOL EXP THER, V96, P99
  • [9] MAYER P, 1983, INFECTION, V11, P15
  • [10] NARITA H, 1990, 30TH INT C ANT AG CH