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新型N-取代7-氨基头孢烷酸衍生物作为抗肺炎链球菌的潜在药物。合成与体外活性

New N-substituted 7-aminocephalosporanic acid derivatives as potential agents against Streptococcus pneumoniae. Synthesis and in vitro activity.

作者信息

Balsamo A, Barontini S, Calvani F, Gentili D, Macchia M, Rossello A, Di Modugno E, Felici A

机构信息

Dipartimento di Scienze Farmaceutiche, Pisa, Italy.

出版信息

Bioorg Med Chem Lett. 1999 Apr 5;9(7):1035-40. doi: 10.1016/s0960-894x(99)00127-4.

Abstract

The synthesis and the antimicrobial properties of a new series of cephalosporinic beta-lactam antibiotics is described. The data reported in the present paper show the potential of this type of substituted cephalosporins as new anti Gram-positive antibiotic drugs. In fact, all compounds tested showed a good in vitro antibacterial activity against the most relevant Gram-positive pathogens including resistant species that currently represent unmet medical need. On the contrary, the new synthesized compounds were found to be completely devoid of any activity on Gram-negative bacteria up to a concentration of the single agent of 128 microg/ml.

摘要

描述了一系列新型头孢菌素类β-内酰胺抗生素的合成及其抗菌特性。本文报道的数据表明,这类取代头孢菌素作为新型抗革兰氏阳性抗生素药物具有潜力。事实上,所有测试的化合物对最相关的革兰氏阳性病原体均表现出良好的体外抗菌活性,包括目前尚未满足医疗需求的耐药菌株。相反,新合成的化合物在单剂浓度高达128微克/毫升时,对革兰氏阴性菌完全没有任何活性。

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