CLAVULANIC ACID, A NOVEL INHIBITOR OF BETA-LACTAMASES
CLAVULANIC ACID, A NOVEL INHIBITOR OF BETA-LACTAMASES
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DOI：
10.1128/aac.14.5.650
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发表时间：
1978-01-01
影响因子：
4.9
通讯作者：
FU, KP
中科院分区：
文献类型：
--
作者：
NEU, HC;FU, KP
克拉维酸，Z-(2R,5R)-3-(。-羟乙基二烯)-7-氧-4-氧-1-氮杂环-[3,2,0]庚烷-2-羧酸被证明是一种有效的。-内酰胺酶的里士满II型，III型，IV型和v型抑制是一个时间依赖性反应，是不可逆的。克拉维酸对金黄色葡萄球菌、肠杆菌科和铜绿假单胞菌的抑菌活性较差，最低抑菌量大于25 . μ g/ml。对淋病奈瑟菌的抑制作用为0.1 μ m。流感嗜血杆菌为6.3 . μ g/ml。克拉维酸与青霉素类和头孢菌素协同抑制β。产生内酰胺酶的金黄色葡萄球菌和肠杆菌科。克拉维酸联用氨苄西林抑制β。-产生内酰胺酶的淋病奈瑟菌、流感嗜血杆菌、大肠杆菌、伤寒沙门氏菌和索内志贺氏菌。
Clavulanic acid, Z-(2R,5R)-3-(.beta.-hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo-[3,2,0]heptane-2-carboxylic acid, was shown to be an effective inhibitor of the .beta.-lactamases of the Richmond types II, III, IV and V. Inhibition is a time-dependent reaction and is irreversible. Clavulanic acid had poor antibacterial activity against Staphylococcus aureus, Enterobacteriaceae and Pseudomonas aeruginosa, with minimal inhibitory levels greater than 25 .mu.g/ml. It did inhibit the majority of Neisseria gonorrhoeae at 0.1 .mu.g/ml and Haemophilus influenzae at 6.3 .mu.g/ml. Clavulanic acid acted synergistically with penicillins and cephalosporins to inhibit .beta.-lactamase-producing S. aureus and Enterobacteriaceae. Clavulanic acid combined with ampicillin inhibited .beta.-lactamase-producing N. gonorrhoeae, H. influenzae, Escherichia coli, Salmonella typhi and Shigella sonnei.