首页> 美国卫生研究院文献>Antimicrobial Agents and Chemotherapy >Use of the chromosomal class A beta-lactamase of Mycobacterium fortuitum D316 to study potentially poor substrates and inhibitory beta-lactam compounds.
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Use of the chromosomal class A beta-lactamase of Mycobacterium fortuitum D316 to study potentially poor substrates and inhibitory beta-lactam compounds.

机译:辅助分枝杆菌D316的A类染色体β-内酰胺酶用于研究潜在的不良底物和抑制性β-内酰胺化合物的用途。

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摘要

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.
机译:测试了十六种通常被认为是β-内酰胺酶稳定或代表潜在的β-内酰胺抑制剂和灭活剂的化合物,以对抗由分枝杆菌产生的β-内酰胺酶。表现出最令人感兴趣的特性的化合物是BRL42715,它是迄今为止最好的灭活剂; CGP31608和头孢他啶,未被酶识别。因此,这些化合物表现出足以抵抗分枝杆菌感染的特性。尽管氯沙西林,双氯西林,头孢西丁和CP65207-2对酶的抑制效果较差,但它们的底物也较差,可能被认为是潜在的抗分枝杆菌药。相反,CGP31523A和头孢他美是良好的底物。

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