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2000
Volume 21, Issue 9
  • ISSN: 1573-4064
  • E-ISSN: 1875-6638

Abstract

Introduction

A series of novel 2-((3,5-diphenylpyrazin-2-yl)amino)-1-(piperidin-1-yl/pyrrolidin-1-yl)ethanone derivatives () were synthesized and evaluated for their tuberculosis activity using the standard strain H37Rv and two other clinically isolated multidrug-resistant strains with different resistances.

Methods

All compounds showed promising results in tuberculosis activity. Among them, and demonstrated remarkable activity at 5 μg/mL against H37Rv and three other MDR strains. The compounds , , and were sensitive, showing inhibition between 15-25 μg/mL against . growth. docking studies were conducted for using the 2FUM protein of .

Results

These studies revealed that compounds and exhibited strong interactions with the MTB protein, with binding energies of -9.85 kcal/mol and -10.74 kcal/mol, respectively, and inhibitory concentrations of 0.38 µM and 0.77 µM.

Conclusion

Moreover, these motifs also displayed good binding energy coupled with favorable minimum inhibitory concentrations (MIC).

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Synthesis, Docking, and Biological Studies of Pyrazine Derivatives as Antimycobacterial Agents
Med. Chem. 21, 1019 (2025); https://doi.org/10.2174/0115734064337815241115050020
/content/journals/mc/10.2174/0115734064337815241115050020
/content/journals/mc/10.2174/0115734064337815241115050020
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  • Article Type:     Research Article
Keyword(s): ADMET; docking studies; H37Rv; MIC; Pyrazine; tuberculosis

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