克拉维酸，一种新型β-内酰胺酶抑制剂。
Clavulanic acid, a novel inhibitor of beta-lactamases.
作者信息
Neu H C, Fu K P
出版信息
Antimicrob Agents Chemother. 1978 Nov;14(5):650-5. doi: 10.1128/AAC.14.5.650.
Abstract
Clavulanic acid, Z-(2R,5R)-3-(beta-hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo-[3,2,0] heptane-2-carboxylic acid, has been 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 mug/ml. It did inhibit the majority of Neisseria gonorrhoeae at 0.1 mug/ml and Haemophilus influenzae at 6.3 mug/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.
摘要
克拉维酸，即Z-(2R,5R)-3-(β-羟基亚乙基)-7-氧代-4-氧杂-1-氮杂双环-[3,2,0]庚烷-2-羧酸，已被证明是里士满II、III、IV和V型β-内酰胺酶的有效抑制剂。抑制作用是一种时间依赖性反应，且是不可逆的。克拉维酸对金黄色葡萄球菌、肠杆菌科细菌和铜绿假单胞菌的抗菌活性较差，最小抑菌浓度大于25μg/ml。它在0.1μg/ml时确实能抑制大多数淋病奈瑟菌，在6.3μg/ml时能抑制流感嗜血杆菌。克拉维酸与青霉素和头孢菌素协同作用，以抑制产β-内酰胺酶的金黄色葡萄球菌和肠杆菌科细菌。克拉维酸与氨苄西林联合使用可抑制产β-内酰胺酶的淋病奈瑟菌、流感嗜血杆菌、大肠杆菌、伤寒沙门菌和宋内志贺菌。
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