Discovery and Optimization of 6-(1-Substituted pyrrole-2-yl)-s-triazine Containing Compounds as Antibacterial Agents

Antimicrobial drug resistance is a major health issueplaguing healthcare worldwide and leading to hundreds ofthousands of deaths globally each year. Tackling this problemrequires discovery and development of new antibacterial agents. Inthis study, we discovered novel 6-(1-substituted pyrrole-2-yl)-s-triazine containing compounds that potently inhibited the growthofStaphylococcus aureusregardless of its methicillin-resistant status,displaying minimum inhibitory concentration (MIC) values as lowas 1 mu M. The presence of a single imidazole substituent was criticalto the antibacterial activity of these compounds. Some of thecompounds also inhibited several nontubercular mycobacteria. Wehave shown that these molecules are potent bacteriostatic agents and that they are nontoxic to mammalian cells at relevantconcentrations. Further development of these compounds as novel antimicrobial agents will be aimed at expanding ourarmamentarium of antibiotics

Automated summary

Antimicrobial drug resistance is a global health issue that results in hundreds of thousands of deaths annually. This study identified novel compounds with potent antibacterial activity against Staphylococcus aureus, including methicillin-resistant strains, with minimum inhibitory concentration as low as 1 μM. Some of these compounds also showed inhibitory effect against nontubercular mycobacteria, and were nontoxic to mammalian cells at relevant concentrations.