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一种新型1-氧杂头孢菌素与其他β-内酰胺类化合物的抗菌活性比较。

Antibacterial activity of a new 1-oxa cephalosporin compared with that of other beta-lactam compounds.

作者信息

Neu H C, Aswapokee N, Fu K P, Aswapokee P

出版信息

Antimicrob Agents Chemother. 1979 Aug;16(2):141-9. doi: 10.1128/AAC.16.2.141.

DOI:10.1128/AAC.16.2.141
PMID:314774
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC352811/
Abstract

The in vitro activity of (6R,7R)-7-{[carboxy(4-hydroxyphenyl)acetyl]amino}-7-methoxy-3-[[(1-methyl -1H-tetrazol-5-yl)thio]methyl]-8-oxo-5-oxa-1-azabicyclo-[4.2.0]oct-2-ene -2-carboxylic acid was tested against isolates of gram-positive and negative bacteria and compared with those of cephalothin, cefuroxime, cefamandole, cefoxitin, cefotaxime, and carbenicillin. The compound was less active than the other compounds when tested against Staphylococcus aureus and Staphylococcus epidermidis. It had equal or slightly less activity than did cefotaxime when tested against members of the Enterobacteriaceae, but was 8- to 32-fold more active than the other cephalosporins against the Enterobacteriaceae, inhibiting most isolates at concentrations less than 0.5 mug/ml. The compound was twofold more active than cefotaxime and cefoxitin against Bacteroides, and it was twofold more active than cefotaxime and fourfold more active than carbenicillin against Pseudomonas aeruginosa. In vitro activity did not correlate with either the presence or type of beta-lactamase in either Enterobacteriaceae or Pseudomonas. The compound showed minimal synergy when combined with aminoglycosides or carbenicillin.

摘要

测试了(6R,7R)-7-{[羧基(4-羟基苯基)乙酰基]氨基}-7-甲氧基-3-[[(1-甲基-1H-四氮唑-5-基)硫代]甲基]-8-氧代-5-氧杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸对革兰氏阳性和阴性细菌分离株的体外活性,并与头孢噻吩、头孢呋辛、头孢孟多、头孢西丁、头孢噻肟和羧苄青霉素进行了比较。该化合物在针对金黄色葡萄球菌和表皮葡萄球菌进行测试时,活性低于其他化合物。在针对肠杆菌科成员进行测试时,其活性与头孢噻肟相当或略低,但对肠杆菌科的活性比其他头孢菌素高8至32倍,在浓度低于0.5μg/ml时能抑制大多数分离株。该化合物对拟杆菌的活性比头孢噻肟和头孢西丁高两倍,对铜绿假单胞菌的活性比头孢噻肟高两倍,比羧苄青霉素高四倍。体外活性与肠杆菌科或假单胞菌中β-内酰胺酶的存在或类型均无相关性。该化合物与氨基糖苷类或羧苄青霉素联合使用时显示出最小的协同作用。

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本文引用的文献

1
Cefamandole, a cephalosporin antibiotic with an unusually wide spectrum of activity.头孢孟多,一种具有异常广泛活性谱的头孢菌素抗生素。
Antimicrob Agents Chemother. 1974 Aug;6(2):177-82. doi: 10.1128/AAC.6.2.177.
2
Cefoxitin, a semisynthetic cephamycin antibiotic: antibacterial spectrum and resistance to hydrolysis by gram-negative beta-lactamases.头孢西丁,一种半合成头孢霉素抗生素:抗菌谱及对革兰氏阴性β-内酰胺酶水解的抗性。
Antimicrob Agents Chemother. 1974 Aug;6(2):170-6. doi: 10.1128/AAC.6.2.170.
3
Novel method for detection of beta-lactamases by using a chromogenic cephalosporin substrate.一种使用显色头孢菌素底物检测β-内酰胺酶的新方法。
Antimicrob Agents Chemother. 1972 Apr;1(4):283-8. doi: 10.1128/AAC.1.4.283.
4
The beta-lactamases of gram-negative bacteria and their role in resistance to beta-lactam antibiotics.革兰氏阴性菌的β-内酰胺酶及其在对β-内酰胺类抗生素耐药性中的作用。
J Antimicrob Chemother. 1976 Jun;2(2):115-57. doi: 10.1093/jac/2.2.115.
5
HR 756, a new cephalosporin active against gram-positive and gram-negative aerobic and anaerobic bacteria.HR 756,一种对革兰氏阳性菌及革兰氏阴性需氧菌和厌氧菌均有活性的新型头孢菌素。
Antimicrob Agents Chemother. 1979 Feb;15(2):273-81. doi: 10.1128/AAC.15.2.273.
6
Cefoxitin: an overview of clinical studies in the United States.
Rev Infect Dis. 1979 Jan-Feb;1(1):233-9. doi: 10.1093/clinids/1.1.233.
7
Activity of HR 756 against Haemophilus influenzae, Bacteroides fragilis and Gram-negative rods.HR 756对流感嗜血杆菌、脆弱拟杆菌和革兰氏阴性杆菌的活性。
J Antimicrob Chemother. 1978 Sep;4(5):445-50. doi: 10.1093/jac/4.5.445.
8
Cefuroxime, a beta-lactamase-resistant cephalosporin with a broad spectrum of gram-positive and -negative activity.头孢呋辛,一种对β-内酰胺酶稳定的头孢菌素,具有广谱的革兰氏阳性和阴性菌活性。
Antimicrob Agents Chemother. 1978 Apr;13(4):657-64. doi: 10.1128/AAC.13.4.657.