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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.

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。

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