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Sch 34343的体外评估:抗菌活性、β-内酰胺酶稳定性及抑制作用

In-vitro evaluation of Sch 34343: antimicrobial activity, beta-lactamase stability and inhibition.

作者信息

Jones R N, Barry A L, Fuchs P C, Thornsberry C

出版信息

J Antimicrob Chemother. 1985 Jun;15 Suppl C:99-109. doi: 10.1093/jac/15.suppl_c.99.

Abstract

Sch 34343 was compared with representative parenteral beta-lactams including monobactams (aztreonam), 1-oxa-beta-lactams (latamoxef), carbapenems (imipenem) and cephalosporins (cefamandole, cefoperazone, cefotaxime, cefsulodin and ceftazidime). Sch 34343 was active against the Enterobacteriaceae (MIC50 range, 0.12-4.0 mg/l) and the facultative Gram-positive cocci (MIC50 range, 0.03-4.0 mg/l), and was comparable to the third-generation cephalosporins and imipenem. Pseudomonas aeruginosa and other Pseudomonas spp. were not susceptible to Sch 34343. Haemophilus influenzae and Neisseria spp. were all susceptible to less than or equal to 2.0 mg/l of Sch 34343. Methicillin-resistant staphylococci (MIC90, 32 mg/l) appear to be insusceptible to Sch 34343. Sch 34343 inhibited the majority of cefotaxime- and gentamicin-resistant bacteria (MICs less than or equal to 8.0 mg/l). The new penem was stable to hydrolysis by 11 beta-lactamase preparations (both plasmid- and chromosomally-mediated types). Sch 34343 inhibited beta-lactamases as did other newer cephalosporins.

摘要

将舒巴坦34343与代表性的肠外β-内酰胺类药物进行了比较,这些药物包括单环β-内酰胺类(氨曲南)、1-氧杂β-内酰胺类(拉氧头孢)、碳青霉烯类(亚胺培南)和头孢菌素类(头孢孟多、头孢哌酮、头孢噻肟、头孢磺啶和头孢他啶)。舒巴坦34343对肠杆菌科细菌(MIC50范围为0.12 - 4.0毫克/升)和兼性革兰氏阳性球菌(MIC50范围为0.03 - 4.0毫克/升)有活性,与第三代头孢菌素和亚胺培南相当。铜绿假单胞菌和其他假单胞菌属对舒巴坦34343不敏感。流感嗜血杆菌和奈瑟菌属对浓度小于或等于2.0毫克/升的舒巴坦34343均敏感。耐甲氧西林葡萄球菌(MIC90为32毫克/升)似乎对舒巴坦34343不敏感。舒巴坦34343抑制了大多数对头孢噻肟和庆大霉素耐药的细菌(MIC小于或等于8.0毫克/升)。这种新型青霉烯对11种β-内酰胺酶制剂(包括质粒介导和染色体介导类型)的水解稳定。舒巴坦34343与其他较新的头孢菌素一样,能抑制β-内酰胺酶。

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