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MK0787(N-甲脒基硫霉素)及其他β-内酰胺类化合物对拟杆菌属的体外活性

In vitro activity of MK0787 (N-formimidoyl thienamycin) and other beta-lactam compounds against Bacteroides spp.

作者信息

Nasu M, Maskell J P, Williams R J, Williams J D

出版信息

Antimicrob Agents Chemother. 1981 Oct;20(4):433-6. doi: 10.1128/AAC.20.4.433.

Abstract

The susceptibilities of 82 strains of the Bacteroides fragilis group to eight beta-lactam compounds, lincomycin, and metronidazole were determined by using an agar dilution technique. MK0787 (N-formimidoyl thienamycin) was the most active compound, inhibiting all strains at a concentration of 1 microgram/ml. Metronidazole was the only other drug of similar activity. Of the beta-lactam compounds, cefoxitin and MK0787 showed uniform activity against all species, whereas most other compounds were relatively less active against Bacteroides distasonis and Bacteroides thetaiotaomicron than against B. fragilis and Bacteroides vulgatus. Using a well diffusion technique, we determined the relative stability of each beta-lactam compound to sonicated cultures of selected resistant strains. Whereas MK0787 was completely stable to inactivation--and with one exception, cefoxitin was also--ceftriaxone, cefotaxime, cephaloridine, and cefoperazone always showed some inactivation, often quite substantial. Moxalactam and ceftazidime were completely stable to some of the enzyme preparations.

摘要

采用琼脂稀释技术测定了82株脆弱拟杆菌属细菌对8种β-内酰胺类化合物、林可霉素和甲硝唑的敏感性。MK0787(N-甲酰亚胺基硫霉素)是活性最强的化合物,在浓度为1微克/毫升时可抑制所有菌株。甲硝唑是唯一具有类似活性的其他药物。在β-内酰胺类化合物中,头孢西丁和MK0787对所有菌种均表现出一致的活性,而大多数其他化合物对解脲拟杆菌和嗜热栖热菌的活性相对低于对脆弱拟杆菌和普通拟杆菌的活性。使用琼脂扩散技术,我们测定了每种β-内酰胺类化合物对所选耐药菌株超声处理培养物的相对稳定性。虽然MK0787对失活完全稳定,且除一例例外头孢西丁也是如此,但头孢曲松、头孢噻肟、头孢啶和头孢哌酮总是表现出一定程度的失活,且往往相当显著。氨曲南和头孢他啶对某些酶制剂完全稳定。

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本文引用的文献

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