MraY-IN-1 (compound 12a) is a potent MraY inhibitor with an IC 50 value of 140 μM. MraY-IN-1 has antimicrobial activity against Escherichia coli K12, Bacillus subtilis W23 and Pseudomonas fluorescens Pf-5 with MIC 50 s of 7 µg/mL, 12 µg/mL and 46 µg/mL, respectively. MraY-IN-1 can be used for researching anti-bacteria.