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利用偶然分枝杆菌D316的染色体A类β-内酰胺酶研究潜在的劣质底物和β-内酰胺抑制性化合物。

Use of the chromosomal class A beta-lactamase of Mycobacterium fortuitum D316 to study potentially poor substrates and inhibitory beta-lactam compounds.

作者信息

Galleni M, Franceschini N, Quinting B, Fattorini L, Orefici G, Oratore A, Frère J M, Amicosante G

机构信息

Laboratory of Enzymology, University of Liège, Belgium.

出版信息

Antimicrob Agents Chemother. 1994 Jul;38(7):1608-14. doi: 10.1128/AAC.38.7.1608.

Abstract

Sixteen different compounds usually considered beta-lactamase stable or representing potential beta-lactam inhibitors and inactivators were tested against the beta-lactamase produced by Mycobacterium fortuitum. The compounds exhibiting the most interesting properties were BRL42715, which was by far the best inactivator, and CGP31608 and ceftazidime, which were not recognized by the enzyme. These compounds thus exhibited adequate properties for fighting mycobacterial infections. Although cloxacillin, dicloxacillin, cefoxitin, and CP65207-2 exhibited poor inhibitory efficiency against the enzyme, they were also rather poor substrates and might be considered potential antimycobacterial agents. By contrast, CGP31523A and ceftamet were good substrates.

摘要

针对偶然分枝杆菌产生的β-内酰胺酶,测试了通常被认为对β-内酰胺酶稳定或代表潜在β-内酰胺抑制剂和灭活剂的16种不同化合物。表现出最有趣特性的化合物是BRL42715(它是迄今为止最好的灭活剂)、CGP31608和头孢他啶(该酶无法识别这两种化合物)。因此,这些化合物具有对抗分枝杆菌感染的足够特性。尽管氯唑西林、双氯西林、头孢西丁和CP65207-2对该酶的抑制效率较差,但它们也是相当差的底物,可能被视为潜在的抗分枝杆菌药物。相比之下,CGP31523A和头孢美特是良好的底物。

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