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Mannich Ketones as Possible Antimycobacterial Agents

机译:Mannich酮作为可能的抗微生物剂

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Twenty-three known unsaturated and fused Mannich ketones and their reduced derivatives (amino alcohols) were selected for an antituberculotic study. They were screened against several mycobacterial strains including Mycobacterium tuberculosis, M. xenopi, and M. gordonae, and minimum inhibitory concentration values were also determined using the standard antituberculotic drug isoniazid (INH) as a reference. Structure-activity relationships were also studied. The mode of action of the test compounds was investigated using transmission electron microscopy, high-performance liquid chromatography, and matrix-assisted desorption/ionization mass spectrometry. Several test substances proved to be as potent as INH, but their antimycobacterial spectra were broader than that of INH. Our findings suggest that their mode of action is probably through the inhibition of mycobacterial cell wall biosynthesis.
机译:选择二十三个已知的不饱和和融合的曼尼希酮及其降低的衍生物(氨基醇)用于抗核酸研究。 它们被筛查针对几种分枝杆菌菌株,包括结核分枝杆菌,M. Xenopi和M. Gordonae,并且还使用标准抗核状药物异唑(INH)确定最小抑制浓度值作为参考。 还研究了结构活动关系。 使用透射电子显微镜,高性能液相色谱和基质辅助解吸/电离质谱来研究测试化合物的作用方式。 几种测试物质被证明是居中的有效性,但它们的抗致细菌光谱比伊纳的抗致细菌光谱更宽。 我们的研究结果表明,它们的作用方式可能是通过抑制分枝杆菌细胞壁生物合成。

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