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1
Epicillin: in vitro laboratory studies.埃匹西林:体外实验室研究。
Infect Immun. 1971 Jul;4(1):44-9. doi: 10.1128/iai.4.1.44-49.1971.
2
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J Infect Dis. 1974 Jun;129(0):suppl:S132-8. doi: 10.1093/infdis/129.supplement_2.s132.
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Beta-lactam antibiotics. I. Comparative structure--activity relationships of 6-acylaminopenicillanic acid derivatives and their 6-(D-alpha-acylaminophenylacetamido) penicillanic acid analogues.β-内酰胺抗生素。I. 6-酰氨基青霉烷酸衍生物及其6-(D-α-酰氨基苯乙酰胺基)青霉烷酸类似物的比较结构-活性关系
J Antibiot (Tokyo). 1974 Dec;27(12):922-30. doi: 10.7164/antibiotics.27.922.
5
[Bacteriological studies of carbenicillin].[羧苄青霉素的细菌学研究]
Jpn J Antibiot. 1972 Feb;25(1):21-7.
6
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引用本文的文献

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Br Med J (Clin Res Ed). 1983 Feb 19;286(6365):583-5. doi: 10.1136/bmj.286.6365.583.
3
Epicillin: experimental chemotherapy, pharmacodynamics, and susceptibility testing.埃皮西林:实验性化疗、药效学及药敏试验
Infect Immun. 1971 Jul;4(1):50-3. doi: 10.1128/iai.4.1.50-53.1971.
4
Newer beta-lactam antibiotics.新型β-内酰胺类抗生素。
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New antibiotics: epicillin, minocycline and spectinomycin a summary of their antibacterial activity, pharmacokinetic properties and therapeutic efficacy.
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Letter: Epicillin in gonorrhoea.信件:用于淋病治疗的埃比西林。
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本文引用的文献

1
A NEW APPROACH TO STUDYING THE PROTEIN-BINDING PROPERTIES OF PENICILLINS.
Nature. 1963 Aug 24;199:758-9. doi: 10.1038/199758a0.
2
The specific hapten of group C (group II alpha) meningococcus. I. Preparation and immunological behavior.C群(Ⅱ组α型)脑膜炎球菌的特异性半抗原。I. 制备及免疫行为
J Immunol. 1958 Oct;81(4):331-6.
3
A new class of semisynthetic penicillins and cephalosporins derived from D-2-(1,4-cyclohexadienyl)glycine.
J Med Chem. 1971 Feb;14(2):117-9. doi: 10.1021/jm00284a008.
4
The binding of antibiotics to serum proteins.抗生素与血清蛋白的结合。
Br J Pharmacol Chemother. 1965 Dec;25(3):638-50. doi: 10.1111/j.1476-5381.1965.tb01788.x.
5
Clinical pharmacology of the new penicillins. 1. The importance of serum protein binding in determining antimicrobial activity and concentration in serum.新型青霉素的临床药理学。1. 血清蛋白结合在决定抗菌活性及血清浓度方面的重要性。
Clin Pharmacol Ther. 1966 Mar-Apr;7(2):166-79. doi: 10.1002/cpt196672166.

埃匹西林:体外实验室研究。

Epicillin: in vitro laboratory studies.

作者信息

Basch H, Erickson R, Gadebusch H

出版信息

Infect Immun. 1971 Jul;4(1):44-9. doi: 10.1128/iai.4.1.44-49.1971.

DOI:10.1128/iai.4.1.44-49.1971
PMID:4343402
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC416262/
Abstract

A new semisynthetic penicillin, structurally related to ampicillin, has been assigned the generic name epicillin, 6-[d-2-amino-2-(1, 4-cyclohexadienyl) acetamido]-penicillanic acid. The antimicrobial spectrum and level of activity of epicillin in vitro are similar to those of ampicillin. In studies with recent clinical isolates, these two antibiotics, when compared with carbenicillin, showed consistently higher antimicrobial activity against Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli, and Proteus species. When tested against Pseudomonas aeruginosa isolates, on the other hand, epicillin exhibited a level of intrinsic activity superior to that of ampicillin but less than that of carbenicillin. Epicillin is an amphoteric substance that is sensitive to penicillinase, is acid-stable, and is minimally, but reversibly, bound to human serum protein.

摘要

一种与氨苄西林结构相关的新型半合成青霉素,已被赋予通用名依匹西林,即6 - [d - 2 - 氨基 - 2 - (1,4 - 环己二烯基)乙酰胺基]青霉烷酸。依匹西林在体外的抗菌谱和活性水平与氨苄西林相似。在对近期临床分离株的研究中,与羧苄西林相比,这两种抗生素对金黄色葡萄球菌、化脓性链球菌、大肠杆菌和变形杆菌属始终表现出更高的抗菌活性。另一方面,在对铜绿假单胞菌分离株进行测试时,依匹西林表现出的内在活性水平高于氨苄西林,但低于羧苄西林。依匹西林是一种两性物质,对青霉素酶敏感,耐酸,与人类血清蛋白的结合程度极低且可逆。