Bacteria are capable of performing a number of biotransformations that may activate or deactivate xenobiotics. Recent efforts have utilized metabolomics techniques to study the fate of small-molecule antibacterials within the targeted organism. Examples involving Mycobacterium tuberculosis are reviewed and analyzed with regard to the insights they provide as to both activation and deactivation of the antibacterial. The studies, in particular, shed light on biosynthetic transformations performed by M. tuberculosis while suggesting avenues for the evolution of chemical tools, highlighting potential areas for drug discovery, and mechanisms of approved drugs. A two-pronged approach investigating the metabolism of antibacterials within both the host and bacterium is outlined and will be of value to both the chemical biology and drug discovery fields.

细菌能够进行多种生物转化，这些转化可以激活或灭活外源性物质。最近的努力利用代谢组学技术来研究小分子抗菌剂在目标生物体内的命运。回顾和分析了涉及结核分枝杆菌的例子，以了解它们对抗菌剂的激活和失活提供的见解。尤其是这些研究揭示了结核分枝杆菌进行的生物合成转化同时提出化学工具发展的途径，突出药物发现的潜在领域以及批准药物的机制。概述了一种研究宿主和细菌内抗菌药物代谢的双管齐下的方法，该方法对化学生物学和药物发现领域都具有价值。