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新型青霉烯抗生素Sch 34343的体外活性、β-内酰胺酶稳定性及抑制特性

In-vitro activity and beta-lactamase stability and inhibitory properties of a new penem antibiotic, Sch 34343.

作者信息

Neu H C, Chin N X, Labthavikul P

出版信息

J Antimicrob Chemother. 1985 Jun;15 Suppl C:25-37. doi: 10.1093/jac/15.suppl_c.25.

Abstract

Sch 34343 is a new penem antibiotic. Its in-vitro activity was determined against Gram-positive and -negative aerobic and anaerobic isolates. Sch 34343 inhibited 90% of strains of Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Salmonella spp, Citrobacter spp. and Shigella spp. at less than 1 mg/1. Ninety per cent of strains of Enterobacter, Morganella and Providencia spp. were inhibited by less than 4 mg/1. Sch 34343 did not inhibit Pseudomonas spp., and it had slightly less activity against Enterobacteriaceae than did cefotaxime or latamoxef (moxalactam), but it inhibited organisms resistant to cefoxitin, cefoperazone and piperacillin. Sch 34343 inhibited methicillin-susceptible Staphylococcus aureus at less than or equal to 0.25 mg/1, and it inhibited haemolytic streptococci at less than or equal to 0.06 mg/1. Sch 34343 inhibited Bacteroides fragilis at 0.06 mg/1, including some cefoxitin-resistant isolates. Sch 34343 was not hydrolysed by plasmid- or chromosomally-mediated beta-lactamases, was an excellent inhibitor of Richmond-Sykes type Ia beta-lactamases, and also inhibited, although less effectively, the common plasmid beta-lactamases. It induced beta-lactamases, but inhibited Enterobacter and Citrobacter spp. in which it induced beta-lactamase activity.

摘要

Sch 34343是一种新型青霉烯类抗生素。测定了其对革兰氏阳性和阴性需氧及厌氧分离菌株的体外活性。Sch 34343在浓度低于1mg/1时可抑制90%的大肠杆菌、肺炎克雷伯菌、奇异变形杆菌、沙门氏菌属、柠檬酸杆菌属和志贺氏菌属菌株。肠杆菌属、摩根氏菌属和普罗威登斯菌属90%的菌株在浓度低于4mg/1时被抑制。Sch 34343不抑制假单胞菌属,其对肠杆菌科细菌的活性略低于头孢噻肟或拉氧头孢(羟羧氧酰胺菌素),但它能抑制对头孢西丁、头孢哌酮和哌拉西林耐药的菌株。Sch 34343在浓度小于或等于0.25mg/1时可抑制甲氧西林敏感金黄色葡萄球菌,在浓度小于或等于0.06mg/1时可抑制溶血性链球菌。Sch 34343在浓度为0.06mg/1时可抑制脆弱拟杆菌,包括一些对头孢西丁耐药的分离菌株。Sch 34343不被质粒或染色体介导的β-内酰胺酶水解,是里士满-赛克斯I a型β-内酰胺酶的优秀抑制剂,并且虽然效果稍差,但也能抑制常见的质粒β-内酰胺酶。它可诱导β-内酰胺酶,但能抑制其诱导β-内酰胺酶活性的肠杆菌属和柠檬酸杆菌属细菌。

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