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半合成青霉素6 -(D(-)-α-羧基-3-噻吩基乙酰胺基)青霉烷酸在体外对假单胞菌有活性。

Semisynthetic penicillin 6-(D(--)-alpha-carboxy-3-thienylacetamido) penicillanic acid active against Pseudomonas in vitro.

作者信息

Neu H C, Winshell E B

出版信息

Appl Microbiol. 1971 Jan;21(1):66-70. doi: 10.1128/am.21.1.66-70.1971.

Abstract

The activity of 6-[d(-)-alpha-carboxy-3-thienylacetamido] penicillanic acid, BRL2288, was determined against Pseudomonas aeruginosa and various gram-negative bacilli. The majority of Pseudomonas strains (89%) were inhibited by 100 mug of the antibiotic per ml. BRL2288 is twofold more active than carbenicillin against Pseudomonas at 100 mug/ml or less. Among Enterobacteriaceae tested, 87% Enterobacter and 87% of Proteus mirabilis strains were inhibited by 25 mug/ml or less. Indole-positive Proteus were inhibited by 10 mug/ml or less. Fifty-five per cent of ampicillin-resistant Escherichia coli were inhibited by 100 mug/ml. Klebsiella were uniformly resistant. BRL2288 is not hydrolyzed by most resistant Pseudomonas, but it is destroyed by the beta-lactamases of E. coli and P. mirabilis. The antibiotic shows synergy with gentamicin but not with penicillinase-resistant penicillins such as cloxacillin. Activity of BRL2288 against gram-positive organisms is two- to eightfold less than that of ampicillin or benzylpenicillin G.

摘要

测定了6 - [d(-)-α-羧基-3-噻吩基乙酰胺基]青霉烷酸(BRL2288)对铜绿假单胞菌和各种革兰氏阴性杆菌的活性。大多数假单胞菌菌株(89%)在每毫升含100微克该抗生素时受到抑制。在每毫升100微克或更低浓度时,BRL2288对假单胞菌的活性比羧苄西林高两倍。在所测试的肠杆菌科细菌中,87%的肠杆菌和87%的奇异变形杆菌菌株在每毫升25微克或更低浓度时受到抑制。吲哚阳性变形杆菌在每毫升10微克或更低浓度时受到抑制。55%的耐氨苄西林大肠杆菌在每毫升100微克时受到抑制。克雷伯菌均具有耐药性。BRL2288不被大多数耐药假单胞菌水解,但会被大肠杆菌和奇异变形杆菌的β-内酰胺酶破坏。该抗生素与庆大霉素显示协同作用,但与耐青霉素酶的青霉素如氯唑西林无协同作用。BRL2288对革兰氏阳性菌的活性比对氨苄西林或苄青霉素G低两至八倍。

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本文引用的文献

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Micro-iodometric assay for penicillinase.青霉素酶的微量碘量法测定
Biochem J. 1962 May;83(2):236-40. doi: 10.1042/bj0830236.
7
Antipseudomonal activity of alpha-sulfoaminopenicillins.α-磺氨基青霉素的抗假单胞菌活性。
Appl Microbiol. 1969 Jun;17(6):881-7. doi: 10.1128/am.17.6.881-887.1969.
8
Use of gentamicin in combinations with other antibiotics.庆大霉素与其他抗生素联合使用。
J Infect Dis. 1969 Apr-May;119(4):370-7. doi: 10.1093/infdis/119.4-5.370.
9
Resistance of Pseudomonas aeruginosa to carbenicillin.铜绿假单胞菌对羧苄青霉素的耐药性。
Lancet. 1969 Apr 12;1(7598):753-4. doi: 10.1016/s0140-6736(69)91754-1.

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