Comparative study of new benzenesulphonamide fluoroquinolones structurally related to ciprofloxacin against selected ciprofloxacin-susceptible and -resistant Gram-positive cocci

被引:11
作者
Alovero, F
Barnes, A
Nieto, M
Mazzieri, MR
Manzo, RH
机构
[1] Univ Nacl Cordoba, Fac Ciencias Quim, Dept Farm, RA-5000 Cordoba, Argentina
[2] Hosp Transito Caceres Allende, Cordoba, Argentina
关键词
D O I
10.1093/jac/48.5.709
中图分类号
R51 [传染病];
学科分类号
100401 ;
摘要
The in vitro activities of benzenesulphonamide fluoroquinolones (BSFQs) I-III, new fluoroquinolones with a p-substituted benzenesulphonyl moiety attached to the C-7 piperazinyl ring of ciprofloxacin, were assessed in comparison with those of N-sulfanilylpiperazinyl fluoroquinolone (NSFQ)-105 and ciprofloxacin for 133 Gram-positive clinical isolates. NSFQ-105 and BSFQ-I were the most active drugs. They were 16- to 64-fold more active than ciprofloxacin against Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis, including ciprofloxacin-resistant strains, and Streptococcus pneumoniae (eight- to 32-fold). A high degree of correlation was found between the MICs of the new compounds and ciprofloxacin for Staphylococcus spp. and E. faecalis. Staphylococci and enterococci exhibit cross-resistance to BSFQs and ciprofloxacin.
引用
收藏
页码:709 / 712
页数:4
相关论文
共 13 条
[1]   IN-VITRO ACTIVITY OF NEW SULPHANILIL FLUOROQUINOLONES AGAINST STAPHYLOCOCCUS-AUREUS [J].
ALLEMANDI, DA ;
ALOVERO, FL ;
MANZO, RH .
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 1994, 34 (02) :261-265
[2]   Mode of action of sulfanilyl fluoroquinolones [J].
Alovero, F ;
Nieto, M ;
Mazzieri, MR ;
Then, R ;
Manzo, RH .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1998, 42 (06) :1495-1498
[3]   Engineering the specificity of antibacterial fluoroquinolones:: Benzenesulfonamide modifications at C-7 of ciprofloxacin change its primary target in Streptococcus pneumoniae from topoisomerase IV to gyrase [J].
Alovero, FL ;
Pan, XS ;
Morris, JE ;
Manzo, RH ;
Fisher, LM .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2000, 44 (02) :320-325
[4]   The fluoroquinolone antibacterials: past, present and future perspectives [J].
Appelbaum, PC ;
Hunter, PA .
INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS, 2000, 16 (01) :5-15
[5]   A review of the comparative in-vitro activities of 12 antimicrobial agents, with a focus on five new 'respiratory quinolones' [J].
Blondeau, JM .
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 1999, 43 :1-11
[6]   In vitro activity of Bay 12-8039, a new 8-methoxyquinolone [J].
Fass, RJ .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1997, 41 (08) :1818-1824
[7]  
Manzo R.H., 1995, Antibacterial 7-[4-[(4-aminophenyl)sulfonyl]-1-piperazinyl]-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid derivatives and synthesis thereof, Patent No. [5395936, US5395936]
[8]  
MANZO RH, 1997, Patent No. 970106669
[9]  
MATZO RH, 1999, Patent No. 253422
[10]  
*NAT COMM CLIN LAB, 1995, METH DIL ANT SUSC TE