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HR916B的活性代谢产物RU29246的体外活性及β-内酰胺酶稳定性比较

Comparative in vitro activity and beta-lactamase stability of RU29246, the active metabolite of HR916B.

作者信息

Yu K W, Chin N X, Neu H C

机构信息

Department of Medicine, College of Physicians & Surgeons, Columbia University, New York, New York 10032.

出版信息

Eur J Clin Microbiol Infect Dis. 1992 Jul;11(7):652-9. doi: 10.1007/BF01961678.

DOI:10.1007/BF01961678
PMID:1396779
Abstract

HR 916B is a new orally absorbed cephalosporin. In tests its active metabolite, RU29246, inhibited Streptococcus pyogenes, Streptococcus agalactiae and Streptococcus pneumoniae at less than or equal to 0.12 micrograms/ml, which is similar to the antibacterial activity of cefuroxime, and was more active than cefaclor. It was also more active (MIC 2 micrograms/ml) than cefixime, cefuroxime, cefaclor and cefotaxime against staphylococci. RU29246 inhibited Escherichia coli, Klebsiella pneumoniae, Citrobacter diversus, Klebsiella oxytoca, Proteus mirabilis, Providencia stuartii and Salmonella spp. at less than or equal to 1 microgram/ml, thus being more active than cefuroxime and cefaclor, but was less active than cefixime and cefotaxime. It did not inhibit Pseudomonas aeruginosa and other Pseudomonas spp., Enterobacter spp., Serratia marcescens or Bacteroides fragilis. RU29246 was not hydrolyzed by TEM-1, Staphylococcus aureus TEM-2 or Moraxella catarrhalis beta-lactamases, but was hydrolyzed by TEM-3 and the chromosomal beta-lactamases of Proteus vulgaris and Morganella morganii. Plasmid and chromosomal beta-lactamases were inhibited by RU29246.

摘要

HR 916B是一种新型口服吸收性头孢菌素。在试验中,其活性代谢产物RU29246对化脓性链球菌、无乳链球菌和肺炎链球菌的抑制浓度小于或等于0.12微克/毫升,这与头孢呋辛的抗菌活性相似,且比头孢克洛更具活性。对于葡萄球菌,它也比头孢克肟、头孢呋辛、头孢克洛和头孢噻肟更具活性(最低抑菌浓度为2微克/毫升)。RU29246对大肠杆菌、肺炎克雷伯菌、异型柠檬酸杆菌、产酸克雷伯菌、奇异变形杆菌、斯氏普罗威登斯菌和沙门氏菌属的抑制浓度小于或等于1微克/毫升,因此比头孢呋辛和头孢克洛更具活性,但比头孢克肟和头孢噻肟活性低。它对铜绿假单胞菌及其他假单胞菌属、肠杆菌属、粘质沙雷氏菌或脆弱拟杆菌无抑制作用。RU29246不被TEM-1、金黄色葡萄球菌TEM-2或卡他莫拉菌β-内酰胺酶水解,但可被TEM-3以及普通变形杆菌和摩根摩根菌的染色体β-内酰胺酶水解。RU29246可抑制质粒和染色体β-内酰胺酶。

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