Identification of novel <i>Mycobacterium tuberculosis</i> leucyl-tRNA synthetase inhibitors with antibacterial activity

BACKGROUND: to existing antibiotics. Therefore, there is an urgent need to discover new antituberculosis agents with unexploited mechanisms of action. The aim of the work was to develop inhibitors of mycobacterial leucyl-tRNA synthetase (LeuRS) with antibacterial activity. MATERIALS AND METHODS: H37Rv strain under four different conditions. RESULTS: values in micromolar range. The most promising compound, N-(5-Benzyl-thiazol-2-yl)-2-[4-(4-methoxy-phenyl)-1H-tetrazol-5-ylsulfanyl]-acetamide, reveals potent antibacterial activity with the best minimum inhibitory concentration (MIC) value of 4.7 µM. CONCLUSION: -(5-Benzyl-thiazol-2-yl)-2-(1-phenyl-1H-tetrazol-5-ylsulfanyl)-acetamide scaffold can be valuable for further biological research and chemical optimization.