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阿洛西林和美洛西林:新型脲基青霉素。

Azlocillin and mezlocillin: new ureido penicillins.

作者信息

Fu K P, Neu H C

出版信息

Antimicrob Agents Chemother. 1978 Jun;13(6):930-8. doi: 10.1128/AAC.13.6.930.

DOI:10.1128/AAC.13.6.930
PMID:677860
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC352365/
Abstract

The activity of azlocillin and mezlocillin, new semisynthetic ureido penicillins, was investigated and compared with that of other known beta-lactam antibiotics. At a concentration of 25 mug/ml, azlocillin inhibited 74% of Enterobacter, 97% of Proteus mirabilis, 64% of Citrobacter, 91% of Pseudomonas aeruginosa, and 82% of Bacteroides strains tested. Mezlocillin inhibited 86% of Shigella, 96% of Enterobacter, 80% of indole-positive Proteus, 88% of Bacteroides, and 63% of Pseudomonas strains tested. Azlocillin was more active against Pseudomonas than was ticarcillin, carbenicillin, or mezlocillin. Mezlocillin was more active than carbenicillin and ampicillin against Escherichia coli, Klebsiella, Enterobacter, Citrobacter, Acinetobacter, Serratia, and Bacteroides. Azlocillin and mezlocillin were less active than cefazolin against beta-lactamase-producing E. coli and Klebsiella strains but more active than cefazolin against Enterobacter, indole-positive Proteus, Acinetobacter, Citrobacter, and Serratia strains. Both compounds showed activity equivalent to that of cefoxitin against Bacteroides isolates. Both agents were destroyed by many of the beta-lactamases from gram-negative organisms.

摘要

对新型半合成脲基青霉素阿洛西林和美洛西林的活性进行了研究,并与其他已知的β-内酰胺类抗生素进行了比较。在浓度为25微克/毫升时,阿洛西林抑制了74%的肠杆菌、97%的奇异变形杆菌、64%的柠檬酸杆菌、91%的铜绿假单胞菌以及82%的受试拟杆菌菌株。美洛西林抑制了86%的志贺菌、96%的肠杆菌、80%的吲哚阳性变形杆菌、88%的拟杆菌以及63%的受试假单胞菌菌株。阿洛西林对假单胞菌的活性比替卡西林、羧苄西林或美洛西林更强。美洛西林对大肠杆菌、克雷伯菌、肠杆菌、柠檬酸杆菌、不动杆菌、沙雷菌和拟杆菌的活性比羧苄西林和氨苄西林更强。阿洛西林和美洛西林对产β-内酰胺酶的大肠杆菌和克雷伯菌菌株的活性比头孢唑林弱,但对肠杆菌、吲哚阳性变形杆菌、不动杆菌、柠檬酸杆菌和沙雷菌菌株的活性比头孢唑林强。这两种化合物对拟杆菌分离株的活性与头孢西丁相当。这两种药物都被许多革兰氏阴性菌产生的β-内酰胺酶所破坏。

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1
Azlocillin and mezlocillin: new ureido penicillins.阿洛西林和美洛西林:新型脲基青霉素。
Antimicrob Agents Chemother. 1978 Jun;13(6):930-8. doi: 10.1128/AAC.13.6.930.
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Activity of azlocillin and mezlocillin against gram-negative organisms: comparison with other penicillins.阿洛西林和美洛西林对革兰氏阴性菌的活性:与其他青霉素类药物的比较。
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Comparison of mezlocillin, piperacillin, Bay k 4999 with carbenicillin and ticarcillin against enterobacteriaceae and Pseudomonas aeruginosa.美洛西林、哌拉西林、Bay k 4999与羧苄西林和替卡西林对肠杆菌科细菌及铜绿假单胞菌的比较。
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In vitro activity of apalcillin compared with that of other new penicillins and anti-Pseudomonas cephalosporins.阿帕西林与其他新型青霉素及抗假单胞菌头孢菌素的体外活性比较。
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Nouv Presse Med. 1982 Feb 4;11(5 Pt 2):318-23.

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J Pharmacokinet Biopharm. 1983 Feb;11(1):5-30. doi: 10.1007/BF01061765.
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本文引用的文献

1
Purification and characterization of penicillinases from Salmonella typhimurium and Escherichia coli.鼠伤寒沙门氏菌和大肠杆菌青霉素酶的纯化及特性研究
Arch Biochem Biophys. 1970 Aug;139(2):278-90. doi: 10.1016/0003-9861(70)90479-0.
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Carbenicillin and hypokalemia.羧苄青霉素与低钾血症
Ann Intern Med. 1973 May;78(5):774-5. doi: 10.7326/0003-4819-78-5-774.
3
Microiodometric determination of beta-lactamase activity.β-内酰胺酶活性的微量碘量法测定
Antimicrob Agents Chemother. 1972 Feb;1(2):94-9. doi: 10.1128/AAC.1.2.94.
4
The hemostatic defect produced by carbenicillin.羧苄青霉素产生的止血缺陷。
N Engl J Med. 1974 Aug 8;291(6):265-70. doi: 10.1056/NEJM197408082910601.
5
Comparative in vitro activity and clinical pharmacology of ticarcillin and carbenicillin.替卡西林和羧苄西林的体外活性及临床药理学比较
Antimicrob Agents Chemother. 1975 Oct;8(4):457-62. doi: 10.1128/AAC.8.4.457.
6
Altered penicillin-binding components in penicillin-resistant mutants of Bacillus subtilis.枯草芽孢杆菌青霉素抗性突变体中青霉素结合成分的改变。
Proc Natl Acad Sci U S A. 1976 Jun;73(6):1816-20. doi: 10.1073/pnas.73.6.1816.
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In vitro synergistic effect of netilmicin, a new aminoglycoside antibiotic.新型氨基糖苷类抗生素奈替米星的体外协同作用
Antimicrob Agents Chemother. 1976 Sep;10(3):511-8. doi: 10.1128/AAC.10.3.511.
8
In vitro study of netilmicin compared with other aminoglycosides.奈替米星与其他氨基糖苷类药物的体外研究。
Antimicrob Agents Chemother. 1976 Sep;10(3):526-34. doi: 10.1128/AAC.10.3.526.