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一种作为β-内酰胺酶抑制剂的砜类β-内酰胺化合物。

A sulfone beta-lactam compound which acts as a beta-lactamase inhibitor.

作者信息

Aswapokee N, Neu H C

出版信息

J Antibiot (Tokyo). 1978 Dec;31(12):1238-44. doi: 10.7164/antibiotics.31.1238.

Abstract

CP-45,899 [3,3-dimethyl-7-oxo-4-thia-1-azabicyclo(3,2,0)heptane-2-carboxylic acid, 4,4-dioxide [2S-(2alpha,5alpha)]] has low intrinsic activity against most Gram-positive cocci, Enterobacteriaceae and Pseudomonas. It inhibits Neisseria at concentrations of 0.1 approximately 6.2 microgram/ml. The combination of CP-45,899 and ampicillin inhibited Staphylococcus aureus and Enterobacteriaceae resistant to ampicillin by virtue of beta-lactamase activity. Combination of CP-45,899 and cephalothin was synergistic less often, and CP-45,899 did not act synergistically with carbenicillin or ticarcillin against Pseudomonas resistant to these agents. CP-45,899 acted synergistically with ampicillin against Bacteroides. Synergy of CP-45,899 and ampicillin was demonstrated at varying concentrations suggesting that it may significantly enlarge the antibacterial activity of ampicillin against resistant bacteria.

摘要

CP - 45,899 [3,3 - 二甲基 - 7 - 氧代 - 4 - 硫杂 - 1 - 氮杂双环(3,2,0)庚烷 - 2 - 羧酸,4,4 - 二氧化物 [2S - (2α,5α)]] 对大多数革兰氏阳性球菌、肠杆菌科细菌和假单胞菌的内在活性较低。它在浓度为0.1至约6.2微克/毫升时可抑制奈瑟菌。CP - 45,899与氨苄西林联合使用可抑制因β - 内酰胺酶活性而对氨苄西林耐药的金黄色葡萄球菌和肠杆菌科细菌。CP - 45,899与头孢噻吩联合使用时协同作用较少见,并且CP - 45,899与羧苄西林或替卡西林联合使用时对耐这些药物的假单胞菌无协同作用。CP - 45,899与氨苄西林联合使用对拟杆菌有协同作用。在不同浓度下均证明了CP - 45,899与氨苄西林的协同作用,这表明它可能会显著扩大氨苄西林对耐药菌的抗菌活性。

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