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新型碳青霉烯类药物RS-533对需氧和厌氧革兰氏阳性及革兰氏阴性菌的体外活性及β-内酰胺酶稳定性

In vitro activity against aerobic and anaerobic gram-positive and gram-negative bacteria and beta-lactamase stability of RS-533, a novel carbapenem.

作者信息

Neu H C, Chin N X, Saha G, Labthavikul P

出版信息

Antimicrob Agents Chemother. 1986 Dec;30(6):828-34. doi: 10.1128/AAC.30.6.828.

Abstract

RS-533 is a novel carbapenem antibiotic. Its activity was compared with that of imipenem and the new cephalosporins, aztreonam, piperacillin, and tobramycin. RS-533 had activity comparable to that of imipenem, inhibiting the majority of the Enterobacteriaceae, streptococci, staphylococci, and Bacteroides species at concentrations of less than or equal to 2 micrograms/ml. RS-533 inhibited Enterobacter cloacae, Citrobacter freundii, and Serratia marcescens resistant to ceftazidime, aztreonam, and cefoperazone, but RS-533 did not inhibit all methicillin-resistant Staphylococcus aureus or Pseudomonas maltophilia. It inhibited tobramycin-resistant members of the Enterobacteriaceae and Pseudomonas aeruginosa. RS-533 was stable against attack by common chromosomal and plasmid-mediated beta-lactamases and was an effective inhibitor of many beta-lactamases.

摘要

RS - 533是一种新型碳青霉烯类抗生素。将其活性与亚胺培南以及新型头孢菌素、氨曲南、哌拉西林和妥布霉素的活性进行了比较。RS - 533的活性与亚胺培南相当,在浓度小于或等于2微克/毫升时能抑制大多数肠杆菌科细菌、链球菌、葡萄球菌和拟杆菌属菌种。RS - 533能抑制对头孢他啶、氨曲南和头孢哌酮耐药的阴沟肠杆菌、弗氏柠檬酸杆菌和粘质沙雷氏菌,但RS - 533不能抑制所有耐甲氧西林金黄色葡萄球菌或嗜麦芽窄食单胞菌。它能抑制肠杆菌科细菌和铜绿假单胞菌中对妥布霉素耐药的菌株。RS - 533对常见染色体介导和质粒介导的β - 内酰胺酶具有稳定性,并且是许多β - 内酰胺酶的有效抑制剂。

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