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A Coumarin-Based Analogue of Thiacetazone as Dual Covalent Inhibitor and Potential Fluorescent Label of HadA in . | LitMetric

A novel coumarin-based molecule, designed as a fluorescent surrogate of a thiacetazone-derived antitubercular agent, was quickly and easily synthesized from readily available starting materials. This small molecule, coined , exhibited a combination of appropriate physicochemical and biological properties, including resistance toward hydrolysis and excellent antitubercular efficiency similar to that of well-known thiacetazone derivatives, as well as efficient covalent labeling of HadA, a relevant therapeutic target to combat . More remarkably, was successfully implemented as an imaging probe that is capable of labeling in a selective manner, with an enrichment at the level of the poles, thus giving relevant insights about the polar localization of HadA in the mycobacteria.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8022203PMC
http://dx.doi.org/10.1021/acsinfecdis.0c00325DOI Listing

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