Evaluation of Genotoxicity of Perchlozone, Antituberculous Drug

Соседова, Л. М.; Vokina, Vera A.; Kapustina, E. A.; Bogomolova, Elena Sergeevna

doi:10.1007/s10517-020-04821-w

Cited by 1 publication

(2 citation statements)

References 5 publications

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“…Later, in 2012, Perchlozone (Figure 1), another compound containing thiosemicarbazone scaffold, was approved in Russia for multi‐drug resistant TB treatment regimen [30] . In spite of the favorable toxicological properties of Perchlozone in preclinical and clinical studies, recent investigations in rats indicated genotoxic activity of the drug [31] . As may be seen, TSC is a promising antimycobacterial motif but there should be improvements in the therapeutic index of the drugs bearing it.…”

Section: Introductionmentioning

confidence: 99%

“…[30] In spite of the favorable toxicological properties of Perchlozone in preclinical and clinical studies, recent investigations in rats indicated genotoxic activity of the drug. [31] As may be seen, TSC is a promising antimycobacterial motif but there should be improvements in the therapeutic index of the drugs bearing it. On the basis of the aforementioned findings, the aim of this work is to further explore the synthetic utility of levoglucosenone, focusing on the development of novel antituberculosis agents derived from this chiral synthon that contains a thiosemicarbazone pharmacophore.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis of Levoglucosenone‐derived Thiosemicarbazones as Promising Antituberculosis Agents

Tsai,

Aira,

Ensinck

et al. 2023

ChemistrySelect

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A series of levoglucosenone‐derived thiosemicarbazones have been designed and synthesized following a simple and straightforward procedure. The in vitro antimycobacterial activity of the full library were evaluated against M. tuberculosis H37Ra, with 4 compounds being active in the 1.9–10.7 μg/mL concentration range. To determine the influence of the thiosemicarbazone fragment, the synthetic precursors were analyzed, as well as 50 structurally diverse triazoles and isoxazoles derived from levoglucosenone. Comparing the observed activities with the levels of cell viability in L929 cells at the MIC, it can be concluded that the derivatives reported in this work represent interesting candidates for further development of promising antituberculosis agents.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%