LasB-IN-1 (compound 5f) is an efficient and orally active inhibitor of LasB (IC50 = 8.7 µM). It effectively inhibits elastase production and biofilm formation in Pseudomonas aeruginosa, while also attenuating inflammatory responses by downregulating MAPK and NF-kappaB pathways. LasB-IN-1 holds potential as a candidate agent against drug-resistant infections.