Synthesis and In Vitro Antibacterial Evaluation of Mannich Base Nitrothiazole Derivatives

Molbank Pub Date : 2024-03-18 DOI:10.3390/m1793
Phelelisiwe S. Dube, Dylan Hart, L. Legoabe, Audrey Jordaan, D. Warner, Richard M. Beteck
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Abstract

Nitrothiazole derivatives have been reported to exhibit activity against aerobic, anaerobic, and microaerophilic bacteria. This activity profile makes the nitrothiazole compound class an ideal lead source against Mycobacterium tuberculosis, which flourishes in varied environments with different oxygen concentrations. In this work, we investigated six nitrothiazole derivatives for antitubercular activity. The compounds exhibited potent activity, with compounds 9 and 10 possessing an equipotent MIC90 value of 0.24 µM. The compounds were investigated for cytotoxicity against HEK293 cells and hemolysis against red blood cells, and they demonstrated no cytotoxicity nor hemolytic effects, suggesting they possess inherent antitubercular activity.
曼尼希碱硝基噻唑衍生物的合成与体外抗菌评估
据报道,硝基噻唑衍生物对需氧、厌氧和微嗜氧细菌具有活性。这种活性特征使硝基噻唑类化合物成为抗结核分枝杆菌的理想线索来源,因为结核分枝杆菌在氧气浓度不同的环境中生长旺盛。在这项工作中,我们研究了六种硝基噻唑衍生物的抗结核活性。这些化合物具有很强的活性,其中化合物 9 和 10 的等效 MIC90 值为 0.24 µM。对这些化合物进行了针对 HEK293 细胞的细胞毒性和针对红细胞的溶血试验,结果表明它们既没有细胞毒性,也没有溶血作用,这表明它们具有固有的抗结核活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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