Discovery of potent anti–tuberculosis agents targeting aminoacyl–tRNA synthetases

Authors

  • G. P. Volynets Institute of Molecular Biology and Genetics, NAS of Ukraine 150, Akademika Zabolotnoho Str., Kyiv, Ukraine, 03143 Author
  • S. A. Starosyla RECEPTOR.AI Boston, MA, USA Author
  • V. G. Bdzhola Institute of Molecular Biology and Genetics, NAS of Ukraine 150, Akademika Zabolotnoho Str., Kyiv, Ukraine, 03143 Author
  • S. M. Yarmoluk Institute of Molecular Biology and Genetics, NAS of Ukraine 150, Akademika Zabolotnoho Str., Kyiv, Ukraine, 03143 Author
  • M. A. Tukalo Institute of Molecular Biology and Genetics, NAS of Ukraine 150, Akademika Zabolotnoho Str., Kyiv, Ukraine, 03143 Author

DOI:

https://doi.org/10.7124/bc.000AFB

Keywords:

<em>Mycobacterium tuberculosis</em>, leucyl–tRNA synthetase, methionyl–tRNA synthetase, inhibitor

Abstract

Aim. The aim of our study was to develop small–molecular inhibitors of M. tuberculosis LeuRS with antibacterial activity. Conclusions. Using in silico approaches we identified several chemical classes of inhibitors targeting M. tuberculosis LeuRS and MetRS with IC50 values in micromolar concentration range. It was found that the most promising compounds which possess antibacterial activity belong to N–benzylidene–N’–thiazol–2–yl–hydrazine derivatives. Therefore, the compounds in this class can be valuable for further biological research and optimization.

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Published

2024-09-10

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Section

Chronicle and Information